CARB 61 |
| The anti-tumor effects of cis-diamminedichloroplatinum(II), or cisplatin, have been effectively used to treat testicular, ovarian, bladder, lung, and stomach cancers since 1978. However, the number of side effects, including renal toxicity, and increased drug-resistance due to thwarting of apoptosis and repair of cisplatin-DNA adducts has prompted the synthesis of many potential drugs. Carbohydrates, with their inherent chirality, play integral roles in intracellular targeting and packaging pathways and may provide a unique way to increase drug solubility while serving as a targeting mechanism for solid tumors tissue. We are synthesizing novel carbohydrate-tethered cisplatin analogs. A mild acetobromination protocol, recently developed by our lab, and a standard glycosidation using alkenyl alcohols followed by OsO4 catalyzed oxoneŽ oxidation delivered carboxyalkyl glycosides. These also serves as a general strategy to activate carbohydrates for tethering to bioactive molecules and surfaces by standard peptide bond forming reactions. Here we will present the synthesis and characterization of novel cisplatin analogs using the above described strategy. |
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General Posters
6:00 PM-8:00 PM, Tuesday, 28 March 2006 Georgia World Congress Center -- Ex. Hall B4, Poster
Division of Carbohydrate Chemistry |