Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I

被引：17

作者：

Guo, Wei ^{[1
]}

Miao, Zhenyuan ^{[1
]}

Sheng, Chunquan ^{[1
]}

Yao, Jianzhong ^{[1
]}

Feng, Hao ^{[1
]}

Zhang, Wannian ^{[1
]}

Zhu, Lingjian ^{[1
]}

Liu, Wenfeng ^{[1
]}

Cheng, Pengfei ^{[1
]}

Zhang, Jing ^{[1
]}

Che, Xiaoying ^{[1
]}

Wang, Wenya ^{[1
]}

Luo, Chuan ^{[1
]}

Xu, Yulan ^{[1
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 06期

基金：

中国国家自然科学基金;

关键词：

Homocamptothecin; 9-Benzylideneamino; Antitumor activity; Synthesis; RING-MODIFIED CAMPTOTHECIN; ANTITUMOR-ACTIVITY; PHASE-I; ANALOGS; DRUGS;

D O I：

10.1016/j.ejmech.2010.01.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 9-benzylideneamino derivatives of homocamptothecin were synthesized via Friedlaender cyclization from our obtained intermediate 5. All the compounds were evaluated for in vitro cytotoxicity against three cancer cell lines (A549, LOVO and MDA-MB-435). Most of these derivatives possessed potent growth inhibitory effect on all the tested cell lines and four compounds (6d, 6f, 6i, 6k) showed higher inhibitory activities with the IC50 values of 2.3 nM-9.8 nM against breast cancer cell than topotecan. As compared to CPT, compound 61 revealed higher topoisomerase I inhibitory activity.

引用

页码：2223 / 2228

页数：6

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