1333389-48-2Relevant academic research and scientific papers
Topoisomerase I-mediated antiproliferative activity of 10-substituted and 12-substituted homocamptothecins
Guo, Wei,Liu, Wenfeng,Zhu, Lingjian,Zhang, Yongqiang,Cheng, Pengfei,Dong, Guoqiang,Zhuang, Chunlin,Yao, Jianzhong,Sheng, Chunquan,Miao, Zhenyuan,Zhang, Wannian
experimental part, p. 1539 - 1549 (2011/11/05)
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. Among the 10-substituted compounds, 8a, 8b, 9b, and 9i showed an equivalent or even more potent activity than the positive control drug topotecan against the lung cancer cell line A-549. Moreover, the hCPT analogues 8a and 8b exhibited a higher topoisomerase I inhibitory activity than CPT at a concentration of 100 μM. Copyright
