Synthesis of camptothecin glycosides by phase transfer-catalysis and its inhibitory activity against topo I.
- Author:
Qing-yong LI
1
;
Ying ZHANG
;
Li-ping YAO
;
Yu-jie FU
;
Yuan-gang ZU
;
Xiao-qiang CHEN
;
Chun-ying ZHENG
Author Information
- Publication Type:Journal Article
- MeSH: Antineoplastic Agents, Phytogenic; chemical synthesis; chemistry; pharmacology; Camptothecin; analogs & derivatives; chemical synthesis; chemistry; pharmacology; DNA Topoisomerases, Type I; metabolism; Glycosides; chemical synthesis; chemistry; pharmacology; Humans; Molecular Conformation; Molecular Structure; Tumor Cells, Cultured; drug effects
- From: Acta Pharmaceutica Sinica 2005;40(12):1116-1121
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo find new anticancer drug based on the structure of 10-hydroxy camptothecin.
METHODSSix 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.
RESULTS AND CONCLUSIONThe 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.
