Phosphate ester derivatives of homocamptothecin: Synthesis, solution stabilities and antitumor activities
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- 作者：Zhenyuan Miao ; Jing Zhang ; Liang You ; Juan Wang ; Chunquan Sheng ; Jiangzhong Yao ; Wannian Zhang ; Hao Feng ; Wei Guo ; Lei Zhou ; Wenfeng Liu ; Linjian Zhu ; Pengfei Cheng ; Xiaoying Che ; Wenya Wang ; Chuan Lu
- 关键词：Homocamptothecins ; Antitumor activity ; Topoisomerase I ; Phosphate
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2010
- 出版时间：1 May 2010
- 年：2010
- 卷：18
- 期：9
- 页码：3140-3146
- 全文大小：502 K
文摘
Homocamptothecins (hCPTs) represents a new promising class of topoisomerase I inhibitors with enhanced stability and superior antitumor activity. Some phosphodiesters and phosphotriesters homocamptothecin derivatives were designed and synthesized based on our previous synthetic route. The cytotoxicity in vitro on three cancer cell lines and antitumor activity in vivo, and inhibitory properties of topoisomerase I of these derivatives were evaluated. Among them compounds 24e and 24f exhibited higher cytotoxic activity than IRT and the former exhibited the best antitumor activity in vivo and solution stability both at pH 7.4 and pH 3.0.