ORGN 151 |
| Described is the discovery of an extraordinary structure-activity relationship between forty-five Sansalvamide A compounds and their potency against colon cancer cell line HT-29. Eleven Sansalvamide A derivatives are significantly more potent than Sansalvamide A peptide. One compound, is ten-fold more potent than Sansalvamide A (IC50=4.5µg/ml versus San A peptide IC50 = 45µg/ml). We present data demonstrating that Sansalvamide A derivatives that contain an exchange of one L-amino acid with a structurally similar D-amino acid in position 2 or position 3 exhibit excellent “drug-like” potency against colon cancer. |
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Asymmetric Reactions and Syntheses, Physical Organic Chemistry, Combinatorial Chemistry, Total Synthesis
8:00 PM-10:00 PM, Sunday, 26 March 2006 Georgia World Congress Center -- Ex. Hall B4, Poster
Division of Organic Chemistry |