[Synthesis of camptothecin glycosides by phase transfer-catalysis and its inhibitory activity against topo I].
OBJECTIVE
To find new anticancer drug based on the structure of 10-hydroxy camptothecin.


METHODS
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.


CONCLUSIONS
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.
Li
Qing-yong
QY
Key Laboratory of Forest Plant Ecology of Northeast Forestry University, Ministry of Education, Harbin 150040, China.
Zhang
Ying
Y
Yao
Li-ping
LP
Fu
Yu-jie
YJ
Zu
Yuan-gang
YG
Chen
Xiao-qiang
XQ
Zheng
Chun-ying
CY
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D006027:Glycosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008968:Molecular Conformation; D015394:Molecular Structure; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D006027:Glycosides; D004264:DNA Topoisomerases, Type I; D002166:Camptothecin