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

被引：58
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.
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收藏
页码：592 / 599
页数：8
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