Bioorganic & Medicinal Chemistry 2006-11-01

Synthesis and antitumor activity of novel 10-substituted camptothecin analogues.

Qingyong Li, Yuangang Zu, Rongzhen Shi, Liping Yao, Yujie Fu, Zhiwei Yang, Lei Li

Index: Bioorg. Med. Chem. 14(21) , 7175-82, (2006)

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Abstract

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.