Author/Authors :
Zhenyuan Miao، نويسنده , , Jing Zhang، نويسنده , , Liang You، نويسنده , , Juan Wang، نويسنده , , Chunquan Sheng، نويسنده , , Jiangzhong Yao، نويسنده , , Wannian Zhang، نويسنده , , Hao Feng، نويسنده , , Wei Guo، نويسنده , , Lei Zhou، نويسنده , , Wenfeng Liu، نويسنده , , Linjian Zhu، نويسنده , , Pengfei Cheng، نويسنده , , Xiaoying Che، نويسنده , , Wenya Wang، نويسنده , , Chuan Luo، نويسنده , , Yulan Xu، نويسنده , , Guoqiang Dong، نويسنده ,
Abstract :
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.
Keywords :
Homocamptothecins , Antitumor activity , Topoisomerase I , Phosphate
