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Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins
LI Dizao * #
College of Pharmacy, State key Laboratory of Medicinal Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, P. R. China
*Correspondence author
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Funding: the Fundamental Research Funds for the Central Universities of China （No.No. 65011141) and the Research Fund for the Doctoral Program of Higher Education of China）
Opened online:16 September 2014
Accepted by: none
Citation: LI Dizao.Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins[OL]. [16 September 2014] http://en.paper.edu.cn/en_releasepaper/content/4608374
 
 
A series of novel 1'(N)-acetic acid esters of 20(S)-camptothecins (CPTs) have been synthesized and all of the esters were assayed for in vitro cytotoxicity against five human cancer cell lines A549, Bel7402, BGC-823, HCT-8 and A2780. The results showed that most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines. Here the synthesis and the in vitro antitumor evaluation of 20-O-linked substituted 1'(N)-acetic acid ester derivatives of CPTs are reported.
Keywords:synthesis; Camptothecins; 1'(N)-acetic acid ester; antitumor; Cytotoxicity
 
 
 

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