Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives
- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 8
- DOI:
- 10.3321/j.issn:0513-4870.2004.08.004
- Key Word:
- 喜树碱酯;合成;抗肿瘤活性;苯氧乙酸;camptothecin ester;synthesis;antitumor activity;phenoxyacetic acid
Abstract： 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 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. 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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