文献类型：期刊文献

英文题名：Naphthalimides and analogues as antitumor agents: A review on molecular design, bioactivity and mechanism of action

作者：Chen, Zhuo[1];Xu, Yufang[1];Qian, Xuhong[1]

机构：[1]East China Univ Sci & Technol, Shanghai Key Lab Chem Biol, Shanghai Key Lab New Drug Design, State Key Lab Bioreactor Engn,Sch Pharm, Shanghai 200237, Peoples R China

年份：2018

卷号：29

期号：12

起止页码：1741

外文期刊名：CHINESE CHEMICAL LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000458223600008)】；

基金：We are grateful for the financial supports from the National Natural Science Foundation of China (No. 20536010), National Key Project for Basic Research (No. 2003CB114400), the Program of Shanghai Subject Chief Scientist and the Science and Technology Foundation of Shanghai.

语种：英文

外文关键词：Naphthalimides; Antitumor; Structure activity relationship; Drug design strategy; Mechanism of action

摘要：In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to enhance their DNA binding affinity and antitumor property thereby. Heterocyclic fused naphthalimides, bis-naphthalimides, non-fused substituted naphthalimides and the carboxamide derivatives were synthesized. For example, thio-heterocyclic fused-naphthalimides were designed and evaluated in comparison with their oxo-heterocyclic fused analogues. Extended or created heterocycle-based skeleton were also developed as antitumor agents. On the other hand, we broaden the design strategy of naphthalimide antitumor agents besides DNA intercalation and topo II poison. We have introduced more drug design methods, such as prodrugs, multitarget drugs, computer-aided drug design, photodynamic therapy. For example, we have got naphthalimide derivatives which inhibited topo II and induced LMP by introducing long alkyl chain and polyamines. Several representative compounds were clarified of their antitumor mechanism of action. In all, our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action. (C) 2018 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.