ORGN 148 |
| 10-Hydroxycamptothecin (HCPT) is a plant alkaloid isolated from the stem wood of the Asian tree, Camptotheca acuminata. This compound has demonstrated significant antitumor activity and less toxicity than camptothecin. It was mainly used in the clinical therapy for lung, uterine, ovarian and head and neck cancers. Due to poor water solubility of HCPT, which was administered as the water-soluble sodium salt of the ring opened carboxylate form of HCPT, its clinic efficiency was low. Derivatives of 10-hydroxycamptothecin bearing 1,2,3-triazoles with lactone ring intact have greater potentials in antitumor activity due to its water solubility and stability at physiological pH. Combined with a novel copper-catalyzed 1,3-dipole addition reaction as the key step, a series of new compounds were synthesized and identified for the first time.
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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 |
