Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives.
- Author:
Xian-dao PAN
1
;
Hong-yan LIU
;
Piao-yang SUN
;
Cheng-gen ZHU
;
Jing YANG
;
Kai-hong YUAN
;
Rui HAN
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Antineoplastic Agents; chemical synthesis; chemistry; pharmacology; Camptothecin; chemical synthesis; chemistry; pharmacology; Cell Line, Tumor; drug effects; Esters; chemistry; Female; Humans; Inhibitory Concentration 50; Liver Neoplasms; pathology; Mice; Mice, Inbred ICR; Molecular Structure; Neoplasm Transplantation; Topotecan; analogs & derivatives; chemical synthesis; chemistry; pharmacology; Tumor Burden; drug effects; Xenograft Model Antitumor Assays
- From: Acta Pharmaceutica Sinica 2004;39(8):591-597
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo improve the profile of 20 (S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed.
METHODSThese derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with 1HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by MTT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H22 in mice.
RESULTSTwelve derivatives of camptothecin ester are new compounds.
CONCLUSIONIn vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H22 mouse liver tumoral model.
