Topoisomerase I??Mediated Antiproliferative Activity of 10??Substituted and 12??Substituted Homocamptothecins

…, W Liu, L Zhu, Y Zhang, P Cheng, G Dong…

Index: Guo, Wei; Liu, Wenfeng; Zhu, Lingjian; Zhang, Yongqiang; Cheng, Pengfei; Dong, Guoqiang; Zhuang, Chunlin; Yao, Jianzhong; Sheng, Chunquan; Miao, Zhenyuan; Zhang, Wannian Chemistry and Biodiversity, 2011 , vol. 8, # 8 p. 1539 - 1549

Full Text: HTML

Citation Number: 4

Abstract

Abstract Homocamptothecin (hCPT) is an E-ring modified camptothecin (CPT) analogue, which showed pronounced inhibitory activity of topoisomerase I. In search of novel hCPT- type anticancer agents, two series of hCPT derivatives were synthesized and evaluated in vitro against three human tumor cell lines. The results indicated that the 10-substituted hCPT derivatives had a considerably higher cytotoxic activity than the 12-substituted ones. ...