| MEDI | Wednesday, 31 August 2005 | ||
7:00 PM-9:00 PM Washington DC Convention Center -- Hall A, Poster | |||
Poster Session | |||
| Sponsored by Nature Reviews Drug Discovery | |||
| Organizer: | David Rotella | ||
| 277 | Synthesis and pharmacological evaluation of a novel orally active factor Xa inhibitor Hidemitsu Nishida, Munetaka Ohkouchi, Takafumi Mukaihira, Fumihiko Saitoh, Yuka Nakamura, Yutaka Miyazaki, Tsutomu Satoh, Masashi Mizuno, Tomoyuki Kamino, Yoshitaka Hosaka, Mikihiko Shinozaki, Tamami Oono, Hiroyuki Muramatsu, Ikuya Shiromizu, Tomokazu Matsusue, Masatsugu Kamiya, Makoto Miyauchi, Tooru Yokoyama, Chihaya Kakinuma, Takuo Ogihara, Kazutoshi Yanagibashi, Yasuo Isomura | ||
| 278 | Synthesis and SAR of 1-aryl-3-arylsulfonyl-2-piperidinone derived inhibitors of coagulation factor Xa Joanne M. Smallheer, Shuaige Wang, Mia L. Laws, Joseph M. Luettgen, Robert M. Knabb, Ruth R. Wexler, Patrick Y. Lam, Mimi L. Quan | ||
| 279 | Preparation of highly potent inhibitors of coagulation factor Xa containing pyrazole-fused bicyclic core structures John M. Fevig, Joseph Cacciola, Joseph Buriak Jr., Yun-Long Li, Donald J. Pinto, Michael Orwat, Robert A. Galemmo, Brian Wells, Richard S. Alexander, Karen A. Rossi, Robert M. Knabb, Joseph M. Luettgen, Pancras C. Wong, Stephen Bai, Ruth R. Wexler, Patrick Y. S. Lam | ||
| 280 | Pyrazole-based factor Xa inhibitors: Synthesis and SAR of analogs containing piperidinyl P4 residues Jennifer X. Qiao, Xuhong Cheng, Joanne M. Smallheer, Donald J. P. Pinto, Robert A. Galemmo, Spencer Drummond, Daniel L. Cheney, Kan He, Joseph M. Luettgen, Robert M. Knabb, Ruth R. Wexler, Patrick Y.S. Lam | ||
| 281 | Discovery of 1-[3-Aminobenzisoxazol-5’-yl]-3-trifluoromethyl-6-[2’-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1’]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808), a potent, efficacious and orally bioavailable inhibitor of blood coagulation factor Xa Michael J. Orwat, John M. Fevig, Mimi L. Quan, Robert A. Galemmo, Eugene Amparo, Richard S. Alexander, Karen A. Rossi, Angela M. Smallwood, Pancras C. Wong, Joseph M. Luettgen, Robert M. Knabb, Steven A. Bai, Kan He, Ruth R. Wexler, Patrick Y.S. Lam, Donald J. P. Pinto | ||
| 282 | Bicyclic pyrazinones as TF-FVIIa inhibitors Wen Jiang, Aaron Schmitt, Jeff Bozarth, Alan Rendina, Anzhi Wei, Xiao Wen, Pancras Wong, Ruth Wexler, Scott Priestley, Xiaojun Zhang | ||
| 283 | A selective FVIIa inhibitor with efficacy in an arterial thrombosis model Indawati De Lucca, Jinglan Zhou, Eddine Saiah, Anzhi Wei, Xiao Wen, Earl Crain, Carol Watson, Pancras Wong, Ruth Wexler, Scott Priestley | ||
| 284 | Antithrombin activation with designed small organic activators: The design of a bicyclic–unicyclic isoquinoline based activator Chandravel Krishnasamy, Gunnar Thor Gunnarsson, Umesh R. Desai | ||
| 285 | Structure-activity relationship (SAR) of pentapeptides and hexapeptides derived from [D-Phe-Pro-D-Arg-P1’-CONH2] tetrapeptides inhibitors for thrombin Cristina C. Clement, Manfred Philipp | ||
| 286 | Potent, selective and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis Yonghan Hu, Martin J. DiGrandi, Xuemei Du, Manus Ipek, Leif M. Laakso, Jianchang Li, Wei Li, Thomas S. Rush, Jean Schmid, Jerauld S. Skotnicki, Steve Tam, Jennifer R. Thomason, Jason S. Xiang, Qin Wang, Jeremy I. Levin | ||
| 287 | P1’ Modified sultam hydroxamates as potent MMP inhibitors Ruowei Mo, Dayton T. Meyer, Zelda R. Wasserman, Karl D. Hardman, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, David D. Christ, James M. Trzaskos, Robert C. Newton, Carl P. Decicco, Robert J. Cherney | ||
| 288 | Potent, selective and orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of novel indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents Zhonghui Lu, Rajan Anand, Richard Liu, Maryanne Covington, Krishna Vaddi, Mingxin Qian, James J-W. Duan, Gregory R. Ott | ||
| 289 | Design and synthesis of remarkably selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of novel benzimidazole P1' moieties Gregory R. Ott, Naoyuki Asakawa, Zhonghui Lu, Rajan Anand, Richard Liu, Maryanne Covington, Krishna Vaddi, Mingxin Qian, James J-W. Duan | ||
| 290 | Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors John L. Gilmore, Bryan W. King, Cathy Harris, Thomas P Maduskuie, Stephen E. Mercer, Rui Quin Liu, Maryane B. Covington, Mingxin Qian, Maria D. Ribadeneria, Krishna G. Vaddi, James M. Trzaskos, Robert C. Newton, Carl P. Decicco, James J -W. Duan | ||
| 291 | Exploration of the TACE S1 pocket: Attempts toward achieving selectivity over MMP family members Jeffrey S. Condon, Alexis Aplasca, Eric Feyfant, Diane Joseph-McCarthy, Jeremy I. Levin, Henry-Georges Lombart, Frank E. Lovering, Kaapjoo Park, Jerauld Skotnicki, LinHong Sun, Qin Wang, Weixin Xu, Congmei Zeng, Yuhua Zhang, Yi Zhu | ||
| 292 | Novel hydroxamates as highly potent TACE inhibitors: Part I – de novo design and discovery of two binding modes Z. Zhu, Robert Mazzola, Brian McKittrick, Lisa Sinning, Daniel Lundell, Xiao-Da Niu, Peter Orth, Zhuyan Guo | ||
| 293 | Discovery of novel hydroxamates as highly potent and selective TACE inhibitiors: Part II – SAR development of mode A inhibitors Z. Zhu, Robert Mazzola, Lisa Sinning, Brian Lavey, Guowei Zhou, James Spitler, Shing-Chun Wong, Peter Orth, Zhuyan Guo, Jianshe Kong, Xian Liang, Jesse Wong, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih, Jing Sun, Shu-Cheng Chen, Xiao-Da Niu, Lee Sullivan, Daniel Lundell | ||
| 294 | Design, parallel chemical synthesis and in vitro characterization of novel hydroxamate-based prostaglandin H2 synthase inhibitors Jean Lee | ||
| 295 | Synthesis of 2,3-bis(nitroxy)propyl esters of naproxen, indomethacin, diclofenac and/or aspirin and pharmacogical evaluation of a novel gastro-protective NMI-1182 as a cyclooxygenase inhibitor endowed with nitric oxide donor (CINOD) Subhash P. Khanapure, Michael E. Augustyniak, Vijay Dhawan, Richard A. Earl, James L. Ellis, Maiko Ezawa, David. S. Garvey, Rick D. Gaston, David. R. Janero, Madhavi G. Murty, David J. Schwalb, William S. Selig, Matthew J. Shumway, Andrzej M. Trocha, Shiow-Jyi Wey, Delano V. Young, Irina S. Zemtseva, L. Gordon Letts | ||
| 296 | Substituted 1-biaryl-1,8-naphtyridin-4-one as potent and selective phosphodiesterase-4 inhibitors Sébastien Laliberté, Daniel Guay, Mario Girard, Pierre Hamel, Richard W. Friesen, France Laliberté, Zheng Huang, Angela Styhler, Joseph A. Mancini | ||
| 297 | 8-Arylquinolines derivatives as potent PDE IV inhibitors Patrick Lacombe, Denis Deschênes, Daniel Dubé, Laurence Dubé, Michel Gallant, Dwight Macdonald, Antony Mastracchio, Hélène Perrier, Zheng Huang, France Laliberté, Joseph A. Mancini, Paul Masson, Myriam Salem, Donald W. Nicholson, Yves Girard | ||
| 298 | Conformationally constrained dipeptidyl peptidase IV inhibitors in the α-aminoacyl amide series Hong Dong, Wallace T. Ashton, Leah B Reigle, Rosemary M. Sisco, Jinyou Xu, Lan Wei, Kathryn A. Lyons, Huaibing He, Barbara Leiting, Joseph K. Wu, Xiaoping Zhang, Reshma A. Patel, Frank Marsilio, Nancy A. Thornberry, Ann E. Weber | ||
| 299 | Design, synthesis, and biological evaluation of fused heterocycle-based beta-amino amides as potent, orally active DPP-IV inhibitors for the treatment of type 2 diabetes Jennifer E. Kowalchick, Dooseop Kim, Liping Wang, Maria Beconi, George Eiermann, Huaibing He, Barbara Leiting, Kathryn A. Lyons, Reshma A. Patel, Sangita B. Patel, Aleksandr Petrov, Giovana Scapin, Joseph K. Wu, Nancy A. Thornberry, Ann E. Weber | ||
| 300 | Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes Ping Chen, Charles G. Caldwell, Robert J. Mathvink, Barbara Leiting, Frank Marsilio, Reshma A. Patel, Xiaoping Zhang, Huaibing He, Kathryn A. Lyons, Nancy A. Thornberry, Ann E. Weber | ||
| 301 | Discovery of potent DPP-IV inhibitors Yixian Chen, Steven Richards, Qi Shuai, Jyoti Patel, David Madar, Hong Yong, Zhonghua Pei, Thomas W. von Geldern, Kenton L. Longenecker, Kent Stewart, Tom Lubben, Steven Ballaron, Mike Stashko, James M. Trevillyan, Hing L. Sham | ||
| 302 | Xanthine mimetics as novel DPP4 inhibitors Ravi Kurukulasuriya, Jeffrey J. Rohde, Bruce G. Szczepankiewicz, Fatima Z. Basha, Kenton Longenecker, Steven Ballaron, J. T. Link, Thomas W. von Geldern, Tom Lubben | ||
| 303 | Acyl thiazolidides-novel potent DPP-IV inhibitors Qi Shuai, Jyoti Patel, Irini Akritopoulou-Zanze, Jurgen Dinges, Paul E. Wiedeman, Zhonghua Pei, Melissa Michmerhuizen, Ethan Hoff, Douglas Kalvin, Thomas W. von Geldern, Tom Lubben, Steven Ballaron, Mike Stashko, Bradley A. Zinker, Stevan W. Djuric, David Beno, Anita Kempf-Grote, Amanda Mika, Tomas Farb, Matthew Perham, Andrew Adler, James Trevillyan, Hing L. Sham | ||
| 304 | Design and synthesis of potent inhibitors of protein tyrosine phosphatase 1b Douglas P. Wilson, Zhao-Kui Wan, Follows Bruce, Steven J. Kirincich, Alessandro F. Moretto, Rajeev Hotchandani, Junjun Wu, Weixin Xu, Diane Joseph-McCarthy, Kenneth Foreman, Dave Erbe, Zhang Yan-Ling, James Tobin, Steve Tam, Jinbo Lee | ||
| 305 | En route to potent PTP1b inhibitors: Discovery of a potent and selective thiophene diacid series Zhao-Kui Wan, Bruce Follows, Steven Kirincich, Douglas P. Wilson, Weixin Xu, Diane Joseph-McCarthy, Kenneth Foreman, Yan-Ling Zhang, Dave Erbe, James Tobin, Steve Tam, Jinbo Lee | ||
| 306 | Paper Withdrawn | ||
| 307 | PTP1b inhibitors: Capturing interactions with Arg24 Junjun Wu, Rajeev Hotchandani, Douglas P. Wilson, Eva Binnun, Alessandro Moretto, Zhao-Kui Wan, Bruce Follows, Steven Kirincich, Michael J Smith, Manus Ipek, Diane Joseph-McCarthy, Kenneth Foreman, Wei-Xin Xu, Yan-Ling Zhang, May Tam, Dave Erbe, James Tobin, Steve Tam, Jinbo Lee | ||
| 308 | Pharmacophore hypothesis for g-secretase inhibitor and application in virtual screening Kristi Yi Fan, Xinyi Huang, Ann Aulabaugh, Eric Gundersen, Haas Kimberly, Boyd L. Harrison, J. Steven Jacobsen, Alan Katz, Anthony Kreft, Robert Martone, Scott C. Mayer, Alex Porte | ||
| 309 | Acylguanidines as small molecule BACE1 inhibitors: Exploration of the S1 pocket Ping Zhou, Rajiv Chopra, Derek C. Cole, Jeffrey S. Condon, Rebecca Cowling, Kristi Fan, Boyd L. Harrison, Yun Hu, Lee D. Jennings, Guixian Jin, Wei Liu, Frank E. Lovering, Michael S. Malamas, Eric S. Manas, Koi M. Morris, Albert J. Robichaud, Mohani N. Sukhdeo, Jim Turner, Junjun Wu, Jonanthan Bard | ||
| 310 | Acylguanidines as small molecule BACE1 inhibitors: Optimization of the S1’ region Mohani N. Sukhdeo, Rajiv Chopra, Derek C. Cole, Rebecca Cowling, John W. Ellingboe, Kristi Yi Fan, Yun Hu, Guixian Jin, Lee D. Jennings, Laura Lin, Mei-Chu Lo, Peter A. Lohse, Michael S. Malamas, Eric S. Manas, William J. Moore, Mary-Margaret O'Donnell, Joseph R. Stock, James Strand, Steven Sukits, Kristine Svenson, M. James Turner, Erik Wagner, Jonathan Bard | ||
| 311 | Acylguanidines as small molecule BACE1 inhibitors: Initial exploration of S1 and S2’ pockets Joseph R. Stock, Rajiv Chopra, Derek C. Cole, Jeffrey S. Condon, Rebecca Cowling, John W. Ellingboe, Yun Hu, Guixian Jin, Laura Lin, Mei-Chu Lo, Frank E. Lovering, Michael S. Malamas, Eric S. Manas, James Strand, Steven Sukits, Kristine Svenson, M. James Turner, Erik Wagner, Junjun Wu, Jonathan Bard | ||
| 314 | Design and synthesis of pyrimidoindolone Caspase-3 inhibitors: Part 2 -- Sulfonamide modifications Lisa M. Havran, Wayne E. Childers Jr., Vasilios Marathias, Ann Aulabaugh, Helen Chan, Seongeun Cho, Rebecca Cowling, Myles Fennel, Boyd L. Harrison, Wah-Tung Hum, Bhupesh Kapoor, Huai-Ping Ling, Ronald L. Magolda, Lidia Mosyak, Albert J. Robichaud, Weixin Xu, Andrew Wood | ||
| 315 | Identification and characterization of 3,4-dihydro-2H-pyrimido(1,2-a)indol-10-ones as caspase inhibitors Paul J Dollings, Ann Aulabaugh, Annette Banker, Helen Chan, Seongeun Cho, Rebecca Cowling, Arlene Dietrich, Li Di, George Ellestad, Myles Fennell, Xinyi Huang, Wah-Tung Hum, Donna Huryn, Guixian Jin, Bhupesh Kapoor, Teresa Kleintop, James LaRocque, Huai-Ping Ling, Vasilios Marathias, Franklin Moy, Susan Petusky, William S Somers, Gregory J. Tawa, Desiree Tsao, Andrew Wood, Weixin Xu | ||
| 316 | Thiophene acyl guanidines as BACE1 inhibitors William R. Solvibile, William F. Fobare, Eric S. Manas, Jonathan Bard, Jim Turner, Yun Hu, Erik Wagner, Albert J. Robichaud, Jerry Sun, Rajiv Chopra, Rebecca Cowling, Guixian Jin, Michael S. Malamas | ||
| 317 | Acylguanidines as inhibitors of BACE-1: Variation of pyrrole ring substituents extending into the S1 and S3 pockets Lee D. Jennings, Derek C. Cole, Joseph R. Stock, Rebecca Cowling, Eric S. Manas, Kristi Yi Fan, Ping Zhou, Michael S. Malamas, Rajiv Chopra, Frank E. Lovering, Erik Wagner, Jim Turner, Yun Hu, Jonathan Bard | ||
| 312 | Design and synthesis of pyrimidoindolone Caspase-3 inhibitors: Part 1 -- Phenoxy modifications Lisa M. Havran, Chae-Koo Dan Chong, Wayne E. Childers Jr., Ann Aulabaugh, Helen Chan, Rebecca Cowling, Myles Fennel, Boyd L. Harrison, Wah-Tung Hum, Bhupesh Kapoor, Huai-Ping Ling, Ronald L. Magolda, Albert J. Robichaud, Andrew Wood | ||
| 313 | Design and synthesis of pyrimidoindolone Caspase -- 3 inhibitors: Part 3-Tricycle modifications Lisa M. Havran, Chae-Koo Dan Chong, Wayne E. Childers Jr., Vasilios Marathias, James J. Bicksler, Ann Aulabaugh, Helen Chan, Seongeun Cho, Rebecca Cowling, Myles Fennel, Boyd L. Harrison, Wah-Tung Hum, Bhupesh Kapoor, Huai-Ping Ling, Ronald L. Magolda, Lidia Mosyak, Albert J. Robichaud, Gregory J. Tawa, Weixin Xu, Mei-Yi Zhang, Andrew Wood | ||
| 318 | Design, synthesis and biological activity of novel quinazolinone-based Caspase 3 inhibitors Alexander Greenfield, Cristina Grosanu, Gregory J. Tawa, Wayne E. Childers Jr., Boyd L. Harrison, Ronald L. Magolda, Albert J. Robichaud, Ann Aulabaugh, Helen Chan, Rebecca Cowling, Myles Fennel, Xinyi Huang, Wah-Tung Hum, Bhupesh Kapoor, Huai-Ping Ling, Andrew Wood | ||
| 319 | A computational methodology for calculating the relative binding free energies of caspase-3 inhibitors Gregory J. Tawa, Paul J Dollings, Wayne E. Childers Jr., Andrew Wood, Weixin Xu, Lidia Mosyak, Rebecca Cowling, Ann Aulabaugh, Bhupesh Kapoor, Huai-Ping Ling, Seongeun Cho, Albert J. Robichaud, Alan H. Katz, William S Somers | ||
| 320 | Caspase binding site differences and prescriptions for pan and selective inhibition Gregory J. Tawa, Paul J Dollings, Wayne E. Childers Jr., Andrew Wood, Weixin Xu, Lidia Mosyak, Albert J. Robichaud, Alan H. Katz, William S Somers | ||
| 321 | Aza-peptide epoxides as inhibitors of caspases: How epoxide stereochemistry and prime side interactions influence reactivity and selectivity Amy J. Campbell, Juliana L. Asgian, Jowita Mikolajczyk, Karen E. James, Zhao Zhao Li, Özlem Dogan Ekici, Guy S. Salvesen, James C. Powers | ||
| 322 | N-Benzyl-isatin sulfonamide analogs as potent and selective caspase-3 inhibitors Robert H Mach, Wenhua Chu, Zun Zhang, Chenbo Zeng, Justin Rothfuss, Zhude Tu, Yunxiang Chu, David E. Reichert, Michael J Welch | ||
| 323 | Discovery of 2-aminopyridine inhibitors of FBPase K. Raja Reddy, Mark D. Erion, Qun Dang, Srinivas R. Kasibhatla, Kevin Fan, M. Rami Reddy, Paul D. van Poelje | ||
| 324 | Paper Withdrawn | ||
| 325 | Thiamine mimetics as inhibitors of enzyme transketolase Indrani Gunawardana, Josh Ballard, Bryan Bernat, Steven A. Boyd, Barb Brandhuber, Kevin Condroski, Jason De Meese, Walter DeWolf, Stephen S. Gonzales, May Han, Tomas Kaplan, Yvan Le Huerou, Christine Lemieux, Todd T. Romoff, Darin Smith, Francis Sullivan, Allen A. Thomas, Solly Weiler, S. Kirk Wright, Guy Vigers | ||
| 326 | Potent and selective thiamine antagonists that inhibit transketolase Todd T. Romoff, Josh Ballard, Bryan Bernat, Steven A. Boyd, Barb Brandhuber, Kevin Condroski, Jason De Meese, Walter DeWolf, Stephen S. Gonzales, Indrani Gunawardana, May Han, Yvan Le Huerou, Patrice Lee, Tomas Kaplan, Christine Lemieux, Robin Pedersen, Jed Pheneger, Greg Poch, Darin Smith, Francis Sullivan, Allen A. Thomas, Solly Weiler, S. Kirk Wright, Guy Vigers | ||
| 327 | Non-charged thiamine analogues as inhibitors of enzyme transketolase Allen A. Thomas, Josh Ballard, Bryan Bernat, Steven A. Boyd, Barb Brandhuber, Kevin Condroski, Jason De Meese, Walter DeWolf, Stephen S. Gonzales, Indrani Gunawardana, May Han, Tomas Kaplan, Yvan Le Huerou, Christine Lemieux, Todd T. Romoff, Francis Sullivan, Solly Weiler, S. Kirk Wright, Guy Vigers, Darin Smith | ||
| 328 | Analogues of azepinomycin as inhibitors of guanase: Synthesis and biochemical evaluation of a transition state analogue of the enzyme-catalyzed reaction Ravi K. Ujjinamatada, Ramachandra S. Hosmane | ||
| 329 | Protein Arginine Deiminase 4: Synthesis of mechanism based inactivators Yuan Luo, Paul R. Thompson | ||
| 330 | Straightforward route to a series of mammalian farnesyltransferase inhibitors based upon a simple ethylenediamine scaffold Erin E. Pusateri, Matthew P. Glenn, Sung-Youn Chang, Said M. Sebti, Andrew D. Hamilton | ||
| 331 | Synthesis of 17 a-benzylestradiol derivatives for steroid sulfatase inhibition Diane Fournier, Donald Poirier | ||
| 332 | Pharmacological characterization of a novel orally active neutrophil elastase inhibitor Akemi Kuromiya, Hiroshi Okazaki, Jun-ichi Tsuji | ||
| 333 | Design and synthesis of novel peptide-based orally active inhibitors of human neutrophil elastase Ryotaro Shiratake, Takashi Deguchi, Yasunao Inoue, Noriyuki Imayoshi, Tomohiko Ueda, Kenji Suzuki, Fuminori Sato | ||
| 334 | Paper Withdrawn | ||
| 335 | Synthesis and evaluation of analogs of sfti-1, potent inhibitors of the type II transmembrane serine protease, matriptase Sheng Jiang, Peng Li, Ya-Qiu Long, Sheau-Ling Lee, Cheng Yong Lin, Robert B Dickson, Peter P. Roller | ||
| 336 | Structure-based design of serine protease inhibitors: Discovery of selective chymase inhibitors containing a novel β-amidophosphonic acid recognition motif M. J. Hawkins, M. N. Greco, E. T. Powell, T. W. Corcoran, L. De Garavilla, J. A. Kauffman, Y. Wang, L. Minor, E. Di Cera, N. Sukumar, Z-W. Chen, A. O. Pineda, F. S. Mathews, Bruce E. Maryanoff | ||
| 337 | Combinatorial library of inhibitors for serine protease plasmin: Binding specificity at S3 and S3' subsites Fengtian Xue, Christopher T. Seto | ||
| 338 | Hitting more than one target: Inhibitors of serine- and metallo-b-lactamases John D. Buynak, Hansong Chen, Sukhakar Ganta, Anjaneyulu Sheri | ||
| 339 | Cell permeable α-ketoamide calpain inhibitors for the treatment of Duchenne Muscular Dystrophy Holger Herzner, Reto Bolliger, Marco Henneböhle, Cyrille Lescop, Hervé Siendt, Philipp Weyermann, Andreas von Sprecher, Alexandre Briguet, Isabelle Cordier-Fruh, Michael Erb, Marc Foster, Josef P. Magyar | ||
| 340 | Structural basis for the differential activity of fumagillin-type inhibitors towards type I and type II human methionine aminopeptidase Anthony Addlagatta, Xiaoyi Hu, Jun O. Liu, Brian W. Matthews | ||
| 341 | Practical synthesis and SAR study of aliskiren: An orally active human renin inhibitor Hua Dong, Zhi-Liu Zhang, Jia-Hui Huang, Rujian Ma, Shu-Hui Chen, Ge Li | ||
| 342 | 2-Acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid – a novel irreversible glutathione reductase inhibitor Laura Carlson, Teresa Seefeldt, Jocqueline Herman, Xiangming Guan | ||
| 343 | 2-Acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylcarbonylamino)phenylcarbamoylsulfanyl]propionic acid and its derivatives as a novel class of glutathione reductase inhibitors Teresa Seefeldt, Chandradhar Dwivedi, Greg Peitz, Jocqueline Herman, Laura Carlson, Zhiling Zhang, Xiangming Guan | ||
| 344 | Design, synthesis and evaluation of 2,3-diaryl-1,4-diazepines as potential antiproliferative agents Ramachandran Ramajayam, Rajani Giridhar, Mange Ram Yadav | ||
| 345 | A potent non-porphyrin class of photodynamic therapeutic agent Michael Hall, William M Gallagher, Donal F. O'Shea | ||
| 346 | Preparation of sulfonylaminocarboxylic acid N-arylamides as potential anti-tumor agents Karl J. Fisher, Courtney A. Reubens, Edward M. Doerffler, Jeff K. Curtis, Matthew M. Abelman, Jennifer Davis Bergthold, Richard D. Gless, Irwin Braude | ||
| 347 | Design, synthesis and biological evaluation of novel small-molecule inhibitors of Bcl-2 and Bcl-xL proteins Guoping Wang, Zaneta Nilolovska-Coleska, Renxiao Wang, Jie Guo, Su Qiu, Wei Gao, Sanjeev Kumar, York Tomita, Shaomeng Wang | ||
| 348 | Small molecule inhibitors of Mdm2 as novel cancer therapeutics: From hit-to-lead generation to lead optimization Kyungjin Kim, Emily Liu, Steven G. Mischke, Andrew Schutt, Lyubomir T. Vassilev, Bingbing Wang | ||
| 349 | Structure-based design of potent, non-peptide small-molecule inhibitors of the MDM2-p53 interaction starting from an inactive lead Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Sanjeev Kumar, Peter P. Roller, York Tomita, Krzysztof Krajewski, Jeffrey R. Deschamps | ||
| 350 | Design and synthesis of novel SCFA-carbohydrate hybrids with anti-cancer properties Kevin J. Yarema, Srinivasa Gopalan Sampathkumar, Mark B. Jones, Kaoru Hida, Prasra Gomutputra, Tony H. Sheh | ||
| 351 | Developing 2,4-diaryl 2,5-dihydropyrroles as a novel class of KSP kinesin inhibitors Kenneth L. Arrington, Robert M. Garbaccio, Mark E. Fraley, Christopher Cox, Paul Coleman, George D. Hartman, William F. Hoffman, Carolyn A. Buser, Joe Davide, Kelly Hamilton, Huber Hans, Nancy E. Kohl, Robert B. Lobell, Michael Schaber, Weikang Tao, Eileen S. Walsh, Lawrence C. Kuo, Thomayant Prueksaritanont, Donald Slaughter, Cathy Shu | ||
| 352 | Novel thiazole compounds that inhibit myosin phosphatase activity and human cancer cell proliferation Scott C Grindrod, Masumi Eto, Milton L. Brown | ||
| 353 | Paper Withdrawn | ||
| 354 | Design, synthesis and evaluation of novel macrocyclic paclitaxel analogs and a de novo paclitaxel mimic Liang Sun, Raphaël Geney, Yuan Li, Kan Ma, Iwao Ojima | ||
| 355 | Hydrophobic derivates of 5-(hydroxymethyl)isophthalic acid that selectively induce apoptosis in leukaemia cells but not in fibroblasts P. Gustav Boije af Gennäs, Anna Galkin, Anu Surakka, Timo Ruotsalainen, Päivi Tammela, Jari Yli-Kauhaluoma, Kaarina Sivonen, Pia Vuorela | ||
| 356 | Organic arsenicals as carcinostatic agents Mingzhang Gao, Ralph A. Zingaro | ||
| 357 | Steroidal antileukemic agents: Synthesis and biological evaluation of a family of 2b-aminoandrostane-3a,17b-diols on HL-60 cells Jenny Roy, Dominic Thibeault, Donald Poirier | ||
| 358 | Dialcohols containing a thiophene core: Synthesis and biological evaluations Brahmi Shukla, Rajesh Kavali, Ravi K. Ujjinamatada, Ramachandra S. Hosmane | ||
| 359 | Synthesis and structure-activity relationships of boronic acid chalcone bioisosteres of combretastatin A-4 Yali Kong, Jolanta Grembecka, Michael C Edler, Ernest Hamel, Milton L. Brown | ||
| 360 | Synthesis and biological activity of combretastatin derivatives Kristin Odlo, Trond Vidar Hansen, Pål Rongved, Jo Klaveness | ||
| 361 | Synthesis and SAR of potent N-substituted pipecolic acid derivatives of hemiasterlin that are very poor substrates for P-glycoprotein-mediated drug efflux Shawn Schiller, Hongsheng Cheng, James J Kowalczyk, Galina Kuznetsov, Bruce A. Littlefield, Diana Liu, Véronique Marceau, Cheryl Rowell, Boris M. Seletsky, Edward M. Suh, Karen TenDyke, Murray Towle, Hu Yang | ||
| 362 | New histone deacetylase inhibitors: Benzamide derivatives with a 2-hydroxyethylamino group Yasuo Nagaoka, Taishi Maeda, Shinichi Uesato | ||
| 363 | Paper Withdrawn | ||
| 364 | Synthesis and evaluation of a new class of disulfide-containing linkers for efficient intracellular release of anticancer agents Jin Chen, Xianrui Zhao, Shuyi Chen, Stanislav Jaracz, Iwao Ojima | ||
| 365 | Structure elucidation of novel chloromethylpyridyl purine nucleoside analogues and related compounds Shashikant Phadtare, Liying Chen, Nageswara Kode | ||
| 366 | Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors Guangyu Zhu, Fanglong Yang, Raghavan Balachandran, Peter Hook, Richard B. Vallee, Dennis P. Curran, Billy W. Day | ||
| 367 | Structure based design and synthesis of core binding factor alpha inhibitors: A new target for anti-leukemic agents Kristin M. Graf, Jolanta Grembecka, Miki Newman, John H. Bushweller, Milton L. Brown | ||
| 368 | Hydrophylic 3-carboranyl thymidine analogues (3CTAs) for boron neutron capture therapy (BNCT) Sureshbabu Narayanasamy, B. T. S. Thirumamagal, Jayaseharan Johnsamuel, Cecilia Carnrot, Ashraf S Al-Madhoun, Guirec Y Cosquer, Youngjoo Byun, Achintya K. Bandyopadhyaya, Staffan Eriksson, Werner Tjarks | ||
| 369 | Liposomal formulations of carboranyl cholesterol derivatives for boron neutron capture therapy (BNCT) B. T. S. Thirumamagal, Xiaobin B. Zhao, Danold W. Golightly, Joseph. M. Backer, Robert J. Lee, Werner Tjarks | ||
| 370 | Synthesis and characterization of new titanium and palladium chloroquine complexes with antitumoral activity Maribel Navarro, Nayarit Prieto-Peña, Miriam Arsenak, Peter Taylor | ||
| 371 | Investigation of 2-acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid’s effect on intracellular glutathione reductase, glutathione, and cell growth with monkey kidney cells Yong Zhao, Teresa Seefeldt, Jocqueline Herman, Laura Carlson, Xiangming Guan | ||
| 372 | Dihydroquinazolinones: Dual action inhibitors of cancer cell proliferation and angiogenesis Gary M. Chinigo, Rachel Leal, Michael Elder, Ernest Hamel, Susan L. Mooberry, Milton L. Brown | ||
| 373 | SC-2-71: A novel small molecule dual inhibitor of human cancer cell proliferation and angiogenesis Akunna M. Iheanacho, Scott M. Capitosti, Todd P. Hansen, Gary M. Chinigo, W. Nathaniel Brennen, Rachel M. Leal, Maiko Sakai, Tamara D. Stoops, Susan L. Mooberry, Robert A Sikes, Carlton A. Cooper, Milton L. Brown | ||
| 374 | Synthesis and anti-cancer activity of 2-(2-benzofuranyl)-3-nitro-4h(1)-benzopyran-4-ones Papa Rao Chebrolu, Rakesh Masna | ||
| 375 | Synthesis and anti-tumor activity of fluorocyclopentenyl-pyrimidines Lak Shin Jeong, Long Xuan Zhao, Mikyung Yun, Won Jun Choi, Sang Kook Lee, Kang Man Lee, Young B Lee, Chang H. Ahn | ||
| 376 | Synthesis and biological evaluation of novel anilinoquinoline c-fms inhibitors Terrence L. Smalley Jr., Wendy Y. Mills, Stanley D. Chamberlain, Lee Kuyper, Sab A. Randhawa, John A. Ray, Vicente Samano, Lloyd Frick | ||
| 377 | Discovery and SAR studies of thienopyridones: A class of small molecule AMPK activators Rajesh R. Iyengar, Gang Zhao, Andrew S. Judd, Lemma Kifle, Ning Cao, William J. Chiou, Barbara L. Cool, Heidi S. Camp, Ernst U. Frevert, Teresa M. Turner, Jinrong Liu, Ye Huang, Kennan C. Marsh, Amanda K. Mika, Matthew A. Perham, Bradley A. Zinker, Hing L. Sham, Philip R. Kym | ||
| 378 | Synthesis and evaluation of hydroxamate derivatives as metal-mediated inhibitors of Csk Xianfeng Gu, Yuehao Wang, Anil Kumar, Gonquin Sun, Keykavous Parang | ||
| 379 | A novel dual inhibitor of HER1 and HER2 protein tyrosine kinases Harold Mastalerz, Pierre Dextraze, Ashvinikumar Gavai, Walter Johnson, Francis Lee, Simone Oppenheimer, Edward Ruediger, James Tarrant, Gregory Vite, Dolatrai Vyas, Tai W. Wong, Guifen Zhang, Hongjian Zhang | ||
| 380 | 4-Arylpyridines as selective c-jun-N-terminal kinase-3 (JNK-3) inhibitors Niklas Plobeck, B-M. Swahn, J. Viklund, Y. Xue | ||
| 381 | Design and synthesis of novel DNA-dependent protein kinase (DNA-PK) inhibitors Olivier R. Barbeau, Bernard T. Golding, Roger J. Griffin, Ian R. Hardcastle, Graeme C. M. Smith, Caroline Richardson | ||
| 382 | Discovery of the VEGFR-2 inhibitor BAY 57-9352: The synthesis and SAR of thieno- and furopyridazine analogs Julie A. Dixon, Warren Brini, Stephen J. Boyer, Frederick Ehrgott, Zhenqui Hong, Harold C. Kluender, Rico C. Lavoie, Xin Ma, Raymond Reeves, Tiffany Turner, Wai Wong, Yanlin Zhang, James Elting, Randall M. Jones, Mark McHugh, Guochang Zhu | ||
| 383 | Discovery of the VEGFR-2 inhibitor BAY 57-9352: Combinatorial synthesis of dianilino phthalazine, thienopyridazine, and furopyridazine analogs Dhanapalan Nagarathnam, Ning Su, T. Joe, H. N. Hatoum-Mokdad, Jacques Dumas, W. C. Wong, C. Brennan, Danielle Holmes, Stephen J. Boyer, Jennifer M. Burke, Julie A. Dixon, X. Ma, Frederick Ehrgott, Y. Zhang, Harold C. Kluender, I. Enyedy, James Elting, Randall M. Jones, Guochang Zhu | ||
| 384 | Discovery of the VEGFR-2 inhibitor BAY 57-9352: The synthesis and SAR of phthalazine and isoquinoline analogs Wendy Lee, Stephen J. Boyer, Catherine R. Brennan, Jennifer M. Burke, William Collibee, Jacques Dumas, Holia Hatoum-Mokdad, Danielle Holmes, Zhenqui Hong, Harold C. Kluender, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su, Wai Wong, James Elting, Randall M. Jones, Mark McHugh, Guochang Zhu | ||
| 385 | Identification and development of azolidinone vinyl-fused benzene derivatives, as potent and selective PI3Kg inhibitors, orally active in models of rheumatoid arthritis Thomas Rueckle, Tania Grippi-Vallotton, Maurizio Maio, David Covini, Vincent Pomel, Fabienne Burgat-Charvillon, Dennis Church, Jeffrey Shaw, Wolfgang Sauer, Jasna Klicic, Vladimir Sherbukhin, Anna Quattropani, Jerome Dorbais, Gwenaelle Desforges, Delphine Valognes, Montserrat Camps, Christian Chabert, Corine Gillieron, Bernard Francon, Dominique Perrin, Didier Leroy, Denise Gretener, Anthony Nichols, Hong Ji, Felix Rintelen, Vittoria Ardissone, Chiara Ferrandi, Pierre-Alain Vitte, Susanna Carboni, Rocco Cirillo, Matthias Schwarz, Christian Rommel | ||
| 386 | Design and synthesis of a novel class of potent and highly isoform selective PI3Kg inhibitors Vincent Pomel, David Covini, Dennis Church, Jeffrey Shaw, Jasna Klicic, Delphine Valognes, Montserrat Camps, Christian Chabert, Corine Gillieron, Bernard Francon, Dominique Perrin, Didier Leroy, Denise Gretener, Anthony Nichols, Pierre-Alain Vitte, Susanna Carboni, Christian Rommel, Matthias Schwarz, Thomas Rueckle | ||
| 387 | Paper Withdrawn | ||
| 388 | Discovery and development of p38 MAP kinase inhibitors derived from pyrrolo[2,1-f][1,2,4]triazines John Hynes Jr., Alaric Dyckman, Tianle Li, Shuqun Lin, Stephen T Wrobleski, Hong Wu, Derek Loo, Kim W McIntyre, Gary L Schieven, Rosemary Zhang, Kathleen M Gillooly, Sidney Pitt, Ding Ren Shen, David J Shuster, Arthur Doweyko, John Sack, Joel C. Barrish, John H. Dodd, Katerina Leftheris | ||
| 389 | Design, synthesis, and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 MAP kinase inhibitors Stephen T Wrobleski, Shuqun Lin, Alaric Dyckman, John Hynes Jr., Tianle Li, Hong Wu, Kim W McIntyre, Gary L Schieven, Rosemary Zhang, Kathleen M Gillooly, Sidney Pitt, Ding Ren Shen, David J Shuster, Arthur Doweyko, John Sack, Joel Barrish, John Dodd, Katerina Leftheris | ||
| 390 | Structure active relationship of substituted imidazo(2,1-b)thiazoles: Novel, selective p38 MAP kinase inhibitors David Vensel, Mark A. Ashwell, Syed M. Ali, V. Antonenko, R. Graceffa, M. Harris, M. Kaselj, E. Kelleher, J. Liu, Jean-Marc Lapierre, Yanbin Liu, M. O'Donnell, R. Selliah, Manish Tandon, W. Wrona, Karen Bresciano, K. Caserta, H. Chan, T. Gannett, S. Jones, P. Leydon, S. Mcdonald, A. Naper, L. Saraswat, A. Tyler, M. Warren, S. Zhu | ||
| 391 | Design, synthesis and biological evaluations of novel substituted imidazooxazoles as potent p38 MAP kinase inhibitors Yanbin Liu, Mark A. Ashwell, Syed M. Ali, V. Antonenko, R. Graceffa, M. Harris, M. Kaselj, E. Kelleher, J. Liu, M. O'Donnell, R. Selliah, Manish Tandon, David Vensel, W. Wrona, Jean-Marc Lapierre, Karen Bresciano, K. Caserta, H. Chan, T. Gannett, S. Jones, P. Leydon, S. Mcdonald, A. Naper, L. Saraswat, A. Tyler, M. Warren, S. Zhu | ||
| 392 | Design, synthesis and SAR of bipyridine derivatives as potent and selective p38 kinase inhibitors Seifu Tadesse, Fang-Tsao Hong, Nuria Tamayo, Lillian Liao, David Powers, Yan-Yan Yudor, Violeta Yu, Ming Wong, Brad Henkle, Scot Middleton, Rashid Syed, Tim Harvey, Randall Hungate, Celia Dominguez | ||
| 393 | Evaluation of p38a inhibitors with improved metabolic stability Daniel M Retz, Gilbert M Rishton, Celia Dominguez, Graham Yang, Scott Middleton, Min Wong, David Powers | ||
| 394 | Synthesis and SAR of 6-(carbocycle)-substituted 2-pyridones as potent and selective p38 kinase inhibitors Fang-Tsao Hong, Seifu Tadesse, Nuria Tamayo, Lillian Liao, Martin Goldberg, Cuo-Qiang Cao, David Powers, Yan-Yan Yudor, Violeta Yu, Ming Wong, Brad Henkle, Scot Middleton, Rashid Syed, Tim Harvey, Randall Hungate, Celia Dominguez | ||
| 395 | Searching for potent CDK2 inhibitors using a variant of the Cope elimination Andrew Henderson, Yuzhu Cheng, Nicola J. Curtin, Jane A. Endicott, Bernard T. Golding, Roger J. Griffin, Ian R. Hardcastle, David R. Newell, Martin E. M. Noble, Lan-Zhen Wang | ||
| 396 | Evolution of CDK2/CyclinA recruitment site small molecule inhibitors from a potent peptide lead Georgette M. Castanedo, Kevin Clark, Shumei Wang, Mengling Wong, Dineli Wickramasinghe, Nerissa Mendoza, James Marsters, Daniel P. Sutherlin | ||
| 397 | 2,4-Diamino-5-ketopyrimidines as potent and selective CDK inhibitors: Further exploration of the 2-amino substituents Binh T. Vu, Xin-jie Chu, Qingjie Ding, Gerald Kaplan, Dave Barkovitz, John Mullin, John Moliterni, Nan Jiang, Sung-sau So, Christine Lukacs, Bradford Graves, Xuefeng Yin, Jianping Chen, Wanda DePinto, Allen Lovey | ||
| 398 | Synthesis of 2,4-diamino-5-ketopyrimidines as novel and potent CDK inhibitors: Utilization of a facile metal/halogen exchange initiated by isopropyl magnesium chloride John Moliterni, Xin-Jie Chu, David Bartkovitz, John Mullin, Qingjie Ding, Binh Vu, Nan Jiang, Gerald Kaplan, Sung-Sau So, Christine Lukacs, Brad Graves, Wanda DePinto, Xuefeng Yin, Yingsi Chen, Allen Lovey, Yi Ren, Ping Wang, Corey Brumsted | ||
| 399 | Design and synthesis of 4-alkylamino-2-anilinoquinazoline as potential antitumor agents Grace Shiahuy Chen, Ming-Hsieh Chuang, Meng-Ling Chen, Tsai-Ni Hsieh, Ji-Wang Chern | ||
| 400 | 2,4-Diamino-5-ketopyrimidines: Synthesis and structure-activity relationships of a series of novel and potent CDK inhibitors Xin-Jie Chu, David Bartkovitz, John Mullin, John Moliterni, Binh T. Vu, Qingjie Ding, Nan Jiang, Gerald Kaplan, Gino Sasso, Sung-Sau So, Christine Lukacs, Bradford Graves, Wanda DePinto, Xuefeng Yin, Yingsi Chen, Allen Lovey | ||
| 401 | Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors Gee Hong Kuo, Alan DeAngelis, Stuart Emanuel, Aihua Wang, Yan Zhang, Peter J. Connolly, Xin Chen, Robert H. Gruninger, Catherine Rugg, Angel Fuentes-Pesquera, Steven A. Middleton, Linda Jolliffe, William V. Murray | ||
| 402 | Chemoselective synthesis of 1,2,4-triazole derivatives using solid-supported reagents as selective inhibitors of cyclin-dependent kinase 4 (Cdk4) Kyungjin Kim, Li Chen, Yingsi Chen, Wanda Depinto, Allen Lovey, Warren McComas, Qing Xiang, Xuefeng Yin | ||
| 403 | Conformationally constrained peptide analogs of CIYKYY as inhibitors of Src tyrosine kinase Guofeng Ye, Anil Kumar, Yuehao Wang, Gongqin Sun, Keykavous Parang | ||
| 404 | N-Heteroaromatic-peptide conjugates as Src kinase inhibitors Anil Kumar, Yuehao Wang, Gonquin Sun, Keykavous Parang | ||
| 405 | Converting a weak peptide inhibitor of Src kinase to potent peptide inhibitors by systemic structural modification Anil Kumar, Yuehao Wang, Gongqin Sun, Keykavous Parang | ||
| 406 | New Src kinase inhibitors Part I: 4-Anilino-7-ethynyl-3-quinolinecarbonitriles Biqi Wu, Ana Carolina Barrios Sosa, Diane H. Boschelli, Frank Boschelli, Erick E. Honores, Jennifer M. Golas, Yanong D. Wang | ||
| 407 | New Src kinase inhibitors Part II: 4-Anilino-7-vinyl-3-quinolinecarbonitriles Erick E. Honores, Ana C. Barrios Sosa, Diane H. Boschelli, Frank Boschelli, Jennifer M. Golas, Yan Wang, Yanong D. Wang, Biqi Wu | ||
| 408 | Discovery of a benzotriazine scaffold as a new class of novel src kinase inhibitors W. Wrasidlo, Elena Dneprovskaia, X. Gong, Glenn Noronha, John Hood, Kathy Barrett, Richard Soll, G. Li, W. Liao, Y. Zhou, Ved P. Pathak | ||
| 409 | Design and synthesis of 4-anilino-3-quinolinecarbonitrile with C-7 substituted amines as potent inhibitors of MEK kinase Minu Dutia, Dan M. Berger, Yan Wang, Nancy Torres, Leïla Abrous, Dennis W. Powell, Robert Mallon, Donald Wojiciechowicz, Steven Kim, Larry Feldberg, Karen Collins | ||
| 410 | New approaches for targeting protein-protein interactions: Dual surface phage-display Indraneel Ghosh, Srivats Rajagopal, Thaddeus J. Smith, Aaron Goldman | ||
| 411 | Small molecule inhibitors against mitochondrial permeability transition pore (mPT) Yong-Qian Wu, Sean Hamilton, Doug Wilkinson, Ling Wei, Larisa Serdyuk, Mike Fuller, J Alt, Joseph Steiner, Larry Williams, Camilo Rojas, Gregory S. Hamilton | ||
| 412 | Isoindolinone based inhibitors of the MDM2-p53 protein-protein interaction Stuart J. Kemp, Ian R. Hardcastle, Shafiq U. Ahmed, Noar A. Atatreh, Paul Barrett, Jane A. Endicott, Bernard T. Golding, Roger J. Griffin, Jan Gruber, Claire Hutton, John Lunec, Martin E. M. Noble, Rebecca J. Reid, Christiane Riedinger, Lynette A. Smyth | ||
| 413 | Development of an allosteric inhibitor of the protein-protein interaction between RUNX1 and CBF beta Michael J. Gorczynski, Miki Newman, Jolanta Grembecka, Yunpeng Zhou, Takeshi Corpora, Jae-Pil Jeon, P. Paul Liu, Mohini Sridharan, Ryan Lilien, Bruce R. Donald, John H. Bushweller, Milton L. Brown | ||
| 414 | 1,2-Oxazines as NO prodrugs Harinath Chakrapani, Eric J. Toone | ||
| 415 | Modeling the binding of DAG-lactones to protein kinase C at the lipid interface Megan L. Peach, Ji-Hye Kang, Yongmei Pu, Nancy E. Lewin, Peter M. Blumberg, Marc C. Nicklaus, Victor E. Marquez | ||
| 416 | Exploration of the sn-1 and sn-2 carbonyl functionalities reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C Ji-Hye Kang, Megan L. Peach, Yongmei Pu, Nancy E. Lewin, Peter M. Blumberg, Victor E. Marquez | ||
| 417 | Synthesis and characterization of p-hydroxyphenobarbital O-glucuronide isolated from mouse urine Adnan Ahmed Kadi, William H. Soine, Michael Hindle | ||
| 418 | Design and synthesis of novel phsophoramidate prodrugs as SH2 domain inhibitors Rong Huang, Richard F. Borch | ||
| 419 | Examination of methoxy- and hydroxy-containing phosphonomethylphenylalanine residues in Grb2 SH2 domain-binding peptides Won Jun Choi, Sang-Uk Kang, Karen M. Worthy, Lakshman Bindu, Robert J. Fisher, Terrence R. Burke Jr. | ||
| 420 | High affinity Grb2 SH2 domain-binding macrocycles derived from ring-closing metathesis of alkenylglycine residues with beta-vinyl phosphotyrosyl mimetics Fa Liu, Shinya Oishi, Rajeshri G. Karki, Zhen-Dan Shi, Karen M. Worthy, Lakshman Bindu, Melissa Maderia, Marc C Nicklaus, Joseph J Barchi Jr., Robert J. Fisher, Terrence R. Burke Jr. | ||
| 421 | Design and synthesis of beta-aminomethylene phosphotyrosyl mimetics and their use in the preparation of macrocyclic Grb2 SH2 domain binding inhibitors Sang Uk Kang, Karen M. Worthy, Lakshman Bindu, Rajeshri G. Karki, Marc C. Nicklaus, Robert J. Fisher, Terrence R. Burke Jr | ||
| 422 | Design, synthesis and biological evaluation of lsofylline (LSF) analogs as a possible treatment for Type 1 diabetes Peng Cui, Meng Chen, Zandong Yang, Jerry.L Nadler, Timothy L. Macdonald | ||
| 423 | Structure activity relationship studies of receptor-selective lysophosphatidic acid antagonists Karen M. Carter, William F. McCalmont, Brian H. Heasley, Kevin R. Lynch, Timothy L. Macdonald | ||
| 424 | Chloroketones as oxygen nucleophiles in the preparation of transcriptional factor inhibitors Vivekananda Reddy Konda, Mauro F. A. Adamo | ||
| 425 | Inhibition of hypoxia inducible factor (HIF) hydroxylases Ana Conejo-Garcia, Benoit M. R. Lienard, Michael McDonough, Luke McNeill, Kirsty Hewitson, Christopher J. Schofield | ||
| 426 | IL-9 stimulates MUC4 transcription in respiratory epithelial cells Gautam Damera, Baoyun Xia, Goverdhan Sachdev | ||
| 427 | Determination of liposome-water partition coefficients of pharmaceutical drugs using a simple laboratory titrator Arno Kraft, Nicola M. Howarth, Rebecca Evans, Agnes A. Yeboah, Leonard Gouzin | ||
| 428 | Functional nanoliter chemical microarray for ultra high throughput screening and kinase profiling Kurumi Y. Horiuchi, Yuan Wang, Scott L. Diamond, Stefan A. Kucharewicz, Haiching Ma | ||
| 429 | Kinetic investigation of hydroxamic acids as ester hydrolysis catalysts for nucleic acid triggered prodrug activation (NATPA) systems Bereket Y. Oquare, J. S. Taylor | ||
| 430 | Syntheses of non-conjugated dienes with nucleic bases attached: Varying the distance between the diene and the nucleic base Fares A. Fares, Rania Shatila, Kamal H. Bouhadir | ||
| 431 | Effects of solvation on the chemistry of amino acid complexes of copper David A. Gallagher, Londa Borer | ||
| 432 | In silico virtual ligand screening as a powerful tool to discover side effects of marketed and novel drugs William H. Bisson, Anton Cheltsov, Jiyun Chen, James T. Dalton, Xiao-kun Zhang, R. Abagyan | ||
| 433 | Biotopology of Huntington's disease Demet Gurel, Okan Gurel | ||
| 434 | Multivalent fertilinβ oligopeptides: The dependence of fertilization inhibition on length and density Younjoo Lee | ||
| 435 | Synthesis of a novel tricyclic nucleobase analogue containing a diimidazodiazepine nucleus with potential selectivity Jules Guei, Ramachandra S. Hosmane | ||
| 436 | Oligomerization of β-cleft cross-linked human hemoglobin: Synthesis, intramolecular cross-linking, and intermolecular coupling studies with polyfunctional organic reagents Hongyi Cai, Timothy A. Roach, Ramachandra S. Hosmane | ||
| 437 | Novel neomycin conjugates for multi-recognition of DNA Bert Willis, Dev P. Arya | ||
| 438 | Novel boron containing gadolinium texaphyrins Achintya K. Bandyopadhyaya, Lamine A. Diop, Werner Tjarks | ||
| 439 | Transcription of a DNA template incorporated with a “fat” nucleotide: Studies of base-pair specificity and primer extension using Klenow fragments exo- and exo+ Ning Zhang, Anila Bhan, Ramachandra S. Hosmane | ||
| 440 | Novel approach for diagnostics of genetic material applying auto-fluorescent N2,N3-etheno-adenosine Bilha Fischer, Einat Sharon | ||
| 441 | Synthesis and biological activity of novel polyhydroxy steroids Katharine L. Bowdy, Branko S. Jursic | ||
| 442 | An approach toward the synthesis of a multifunctional organic reagent to effect simultaneous intramolecular cross-link and intermolecular cross-bridge between two molecules of hemoglobin Margaret Dabek, Timothy A Roach, Ramachandra S. Hosmane | ||
| 443 | Synthetic high affinity ligands: Molecular targeting agents Saphon Hok, Rod L. Balhorn, Michael E. Colvin, Michele H. Corzett, Monique Cosman, Gerald L. DeNardo, Sally J. DeNardo, Cheryl E. Dolan, Leslie M. Hanna, Edmond Y. Lau, Felice C. Lightstone, Arutselvan Natarajan, Julie Perkins | ||
| 444 | Inhibition of protein glycation by Rutin’s metabolites Ihab F Halaweish, Daniel Cervantes Laurean, Fathi T Halaweish | ||
| 445 | Incorporation of boronic acid fluorescent reporters into DNA for aptamer selection Na Lin, Zhen Huang, Craig Altier, Lynette Johnston, Nicolas Carrasco, Hao Fang, Jun Yan, Siming Wang, Binghe Wang | ||
| 446 | Design, synthesis and evaluation of conformationally restricted Smac mimetics as inhibitors of IAP family proteins Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Sanjeev Kumar, Wei Gao, Su Qiu, Jianfeng Lu, York Tomita, Peter P. Roller, Shaomeng Wang | ||
| 447 | Synthesis and biological evaluation of all α-hydroxyfarnesylphosphonate geometric isomers on RAS farnesylation José S. Yu, Andrew J. Wiemer, Raymond J. Hohl, David F. Wiemer | ||
| 448 | Imidazole—dioxolane compounds as heme oxygenase inhibitors with enhanced selectivity for HO-1 Jason Z. Vlahakis, Robert T. Kinobe, James F. Brien, Kanji Nakatsu, Walter A. Szarek | ||
| 449 | Design and synthesis of stealth polymeric nanospheres and applications to the delivery of bioactive agents Oluyomi A. Okunola, Emmanuel O. Akala | ||
| 450 | Synthesis and biological evaluation of novel heterocyclic compounds as SMN2 promoter activators for the potential treatment of spinal muscular atrophy J. Singh, J Thurmond, B Pease, M Rao, M Palomo, G Pai, L Bedell, M Keyvan, R Mishra, J Zhang, E Onua, E Bjarnadottir, M Haraldsson, T Andresson, T Gunnseinsdottir, P Atlason, G Sigthorsson, G Bragason, M Thorsteinsdottir, M Gurney | ||
| 451 | Synthesis and polymerization of a functionalized caprolactone monomer for biomedical applications J. Michelle Leslie, Rajesh Kumar Mishra, Edward Turos | ||
| 452 | Development of SPECT imaging agents for the peripheral benzodiazepine receptor Idriss Bennacef, Coliin N. Haile, Andrei O. Koren, J.K. Staley, Ronald M. Baldwin, frederic Bois, Anne Schmidt, Gilles D Tamagnan | ||
| 453 | Synthetic approaches to cell proliferation inhibitors Sarah L Rawe, Violeta Zaric, Kathy M O' Boyle, Paul V Murphy | ||
| 454 | Multi-step preparation of PET imaging probes in integrated microfluidic circuits Guodong Sui, Cheng-Chung Lee, Nagichettiar Satyamurthy, James R. Heath, Michael E. Phelps, Stephen R. Quake, Hsian-Rong Tseng | ||
| 455 | Structure-activity relationship study of IMPY derivatives as candidate radioligands for β-amyloid Lisheng Cai, Lisa Nichols, Jessica Cuevas, Sebastian Temme, Mary M. Herman, Robert B. Innis, Victor W. Pike | ||
| 456 | Synthesis and antimicrobial properties of novel C-6 alkoxycarbamate ketolides Xiaodong Xu, Todd Henninger, Darren Abbanat, Karen Bush, Barbara Foleno, Jamese Hilliard, Mark Macielag | ||
| 457 | Synthesis of 4-position hydrophilic derivatives of thiolactomycin as antitubercular agents Pilho Kim, Yong-Mei Zhang, Gautham Shenoy, Ujjini Manjunatha, Helena Boshoff, Quynh-Anh Nguyen, Michael Goodwin, Darcie Miller, Stephen W. White, Ken Duncan, Charles O. Rock, Clifton E. Barry III, Cynthia S. Dowd | ||
| 458 | Synthesis and binding profile of a novel series of (S)-2b-substituted-4’,4”-difluorobenztropine analogs Mu-Fa Zou, Jianjing Cao, Theresa Kopajtic, Raj Desai, Jonathan L. Katz, Amy H. Newman | ||
| 459 | Microwave-enhanced nucleophilic fluorination in the synthesis of fluoropyridyl derivatives of [3,2-c]pyrazolo-corticosteroids Michael G.C. Kahn, Emmanuel Konde, Francis Dossou, Robert M. Hoyte | ||
| 460 | Focused design and synthesis of novel neuroprotectors (cognition-enhancers) in series of glutamate receptors ligands Nikolay S. Zefirov, Sergey O. Bachurin | ||
| 461 | 6 Angstroms role in opioid receptor agonist analgesics Lin Hu, Hanhong Xu, Gang Hu | ||
Symposium Grid -- Division of Medicinal Chemistry -- Session Listing
The 230th ACS National Meeting, in Washington, DC, Aug 28-Sept 1, 2005