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Synthesis and antitumor activity of novel 10-substituted camptothecin analogues

Authors :
Li, Qingyong
Zu, Yuangang
Shi, Rongzhen
Yao, Liping
Fu, Yujie
Yang, Zhiwei
Li, Lei
Source :
Bioorganic & Medicinal Chemistry. Nov2006, Vol. 14 Issue 21, p7175-7182. 8p.
Publication Year :
2006

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
09680896
Volume :
14
Issue :
21
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
22472509
Full Text :
https://doi.org/10.1016/j.bmc.2006.06.061