Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: Design, synthesis and potential antitumor activity

被引：57

作者：

Wu, Aibin ^{[1
]}

Xu, Yufang ^{[1
]}

Qian, Xuhong ^{[1
]}

机构：

[1] E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 02期

基金：

中国国家自然科学基金; 国家高技术研究发展计划(863计划);

关键词：

Naphthalimide; Leucine; Antitumor; MCF-7; DNA-BINDING; BIOLOGICAL EVALUATION; EFFICIENT ANTITUMOR; AMONAFIDE; AGENTS; ANTICANCER; DERIVATIVES; COMPLEXES; ANALOGS; THIAZONAPHTHALIMIDES;

D O I：

10.1016/j.bmc.2008.11.080

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel naphthalimide derivatives with flexible leucine side chains were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had moderate antitumor activities with the IC50 values of 10 (6) - 10 (5) M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：592 / 599

页数：8

共 59 条

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