Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin

doi:10.6023/cjoc201307049Z

Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (1): 155-160.DOI: 10.6023/cjoc201307049Z Previous Articles Next Articles

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10-羟基喜树碱氨基酸缀合物的合成及抗肿瘤活性研究

孟光荣^a, 李嘉俊^a, 王国林^b, 董孟杰^b, 张倩^a

a 复旦大学药学院药物化学教研室上海 201203;
b 浙江大学附属一院PET中心杭州 310003

收稿日期:2013-08-04 修回日期:2013-08-30 发布日期:2013-09-17
通讯作者: 张倩 E-mail:zhangqian511@shmu.edu.cn
基金资助:
国家自然科学基金（No. 30870730）资助项目.

Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin

Meng Guangrong^a, Li Jiajun^a, Wang Guolin^b, Dong Mengjie^b, Zhang Qian^a

a Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203;
b Positron Emission Tomography Center, First Affiliated Hospital, Zhejiang University, Hangzhou 310003

Received:2013-08-04 Revised:2013-08-30 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

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Meng Guangrong, Li Jiajun, Wang Guolin, Dong Mengjie, Zhang Qian. Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin[J]. Chin. J. Org. Chem., 2014, 34(1): 155-160.

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10-羟基喜树碱氨基酸缀合物的合成及抗肿瘤活性研究

Synthesis and Cytotoxic Activities of the Amino Acid-Conjugates of 10-Hydroxycamptothecin

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