Chinese Journal of Organic Chemistry >
Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin
Received date: 2013-08-04
Revised date: 2013-08-30
Online published: 2013-09-17
Supported by
Project supported by the National Natural Science Foundation of China (No. 30870730).
A series of amino acid-conjugates of 10-hydroxycamptothecin and 9-nitro-10-hydroxycamptothecin were synthesized by means of a two-carbon side chain from 10-hydroxycamptothecin. The cytotoxic activities of all the synthetic compounds on KB, HepG2 and C26 in vitro were evaluated by CCK-8 assay. The results revealed that part of the conjugates exhibit potent anti-proliferative activities against selected tumor cell lines. Among them, the amino acid-conjugates of 10-hydroxycamptothecin show more potent activities than those of 9-nitro-10-hydroxycamptothecin in vitro as antitumor agents.
Key words： camptothecin; amino acid-conjugates; cytotoxic activities
Meng Guangrong , Li Jiajun , Wang Guolin , Dong Mengjie , Zhang Qian . Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin[J]. Chinese Journal of Organic Chemistry, 2014 , 34(1) : 155 -160 . DOI: 10.6023/cjoc201307049Z
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