ABSTRACT
<p><b>AIM</b>To find new anticancer drug based on the structure of 10-hydroxy camptothecin.</p><p><b>METHODS</b>Six camptothecin glycosides (7-12) were synthesized by phase transfer catalysis. The structures of all compounds synthesized were determined by 1H NMR, IR and MS. Their antitumor activity was evaluated on cancer cells in vitro, and inhibitory activity against Topo I was evaluated by molecular biologic method.</p><p><b>RESULTS AND CONCLUSION</b>The result indicated that the yield of camptothecin glycosides by phase transfer catalysis is much higher than by the method from literature, camptothecin glycosides have much lower cytotoxicities on cancer cell in vitro, but have better inhibitory activity of topo I.</p>
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Camptothecin , Chemistry , Pharmacology , DNA Topoisomerases, Type I , Metabolism , Glycosides , Chemistry , Pharmacology , Molecular Conformation , Molecular Structure , Tumor Cells, CulturedABSTRACT
<p><b>AIM</b>To find new anticancer drug based on the structure of 10-hydroxy camptothecin.</p><p><b>METHODS</b>Seven camptothecin derivatives (3 -9) were synthesized and the antitumor activities of these derivatives were evaluated.</p><p><b>RESULTS</b>Structures of seven new compounds were determined by 1HNMR, IR, MS. Seven compounds showed inhibitory effects on Hela, BEL-7402, 7901 cell lines in vitro. Especially, compound 4 showed high bioactivities to all of the tumor cells in vitro, its anticancer activity against human cervical carcinoma Hela was much higher than that of 10-hydroxy camptothecin.</p><p><b>CONCLUSION</b>Some compounds are worth further studying.</p>