- Synthesis and antitumor activity of novel 10-substituted camptothecin analogues.
Synthesis and antitumor activity of novel 10-substituted camptothecin analogues.
Bioorganic & medicinal chemistry (2006-07-28)
Qingyong Li, Yuangang Zu, Rongzhen Shi, Liping Yao, Yujie Fu, Zhiwei Yang, Lei Li
PMID16870453
초록
In an attempt to improve the antitumor activity and decrease the cytotoxicity of camptothecin, 18 new 10-substituted camptothecin derivatives were prepared. The cytotoxicity in vitro on cancer cell lines and antitumor activity in vivo, and inhibitory properties of topoisomerase I of these derivatives were evaluated. Most of these derivatives possessed lower cytotoxicities than CPT, and the compounds 13, 21, 22, 23, and 24 showed similar topoisomerase I inhibitory activity to CPT. Analogues 13 exhibited the best antitumor activity in vivo among all derivatives we prepared.