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Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives

Pan, X-dao.; Liu, H-yan.; Sun, P-yang.; Zhu, C-gen.; Yang, J.; Yuan, K-hong.; Han, R.

Yao Xue Xue Bao 39(8): 591-597

2004

ISSN/ISBN: 0513-4870
PMID: 15563058
Document Number: 572311
Aim To improve the profile of 20 (S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed. Methods These derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with1 HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by WIT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H22 in mice. Results Twelve derivatives of camptothecin ester are new compounds. Conclusion In vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H22 mouse liver tumoral model.

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