1268700-89-5Relevant academic research and scientific papers
Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors
Zhu, Lingjian,Zhang, Xianghua,Lei, Ning,Liu, Wenfeng,Miao, Zhenyuan,Zhuang, Chunlin,Sheng, Chunquan,Guo, Wei,Dong, Guoqiang,Yao, Jianzhong,Cheng, Pengfei,Zhang, Wannian
, p. 1084 - 1094 (2012/09/22)
Homocamptothecin (hCPT) is a camptothecin (CPT) derivative with a seven-membered β-hydroxylactone E ring, which shows higher lactone stability and improves topoisomerase I (Topo I) inhibition activity. In an attempt to improve the antitumor activity of homocamptothecins, a series of 7- alkenyl-homocamptothecin derivatives was designed and synthesized based on a semisynthetic route starting from CPT. Most of the synthesized compounds exhibit higher cytotoxic activities on the A-549 tumor cell line than topotecan (TPT). Some compounds such as 2a and 2o show a broad in vitro antitumor spectrum and exhibit superior Topo I-inhibition activity.
