Synthesis and cytotoxicity of novel 20-O-linked homocamptothecin ester derivatives as potent topoisomerase I inhibitors

Abstract

In an attempt to improve the antitumor activity of homocamptothecins (hCPTs), a series of novel 20-O-linked hCPT ester derivatives were first designed and synthesized based on a synthetic route, by which hCPTs are acylated with different substituted phenoxyacetic acid ester derivatives. Most of the derivatives were assayed for in vitro cytotoxicity against six human cancer cell lines KB, KB/VCR, A549, HCT-8, Bel7402, and A2780, and most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines especially on KB.

Keywords::

• 20-O-linked homocamptothecin ester
• synthesis
• cytotoxicity

Acknowledgments

This research was supported in part by the Fundamental Research Funds for the Central Universities of China (Grant No. 65011141) and the Research Fund for the Doctoral Program of Higher Education of China (Grant No. 20110031120048).