文献类型：期刊文献

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

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

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

机构：[1]State Key Laboratory of Bioreactor Engineering,Shanghai Key Laboratory of Chemical Biology,Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology

年份：2018

卷号：29

期号：12

起止页码：1741

中文期刊名：Chinese Chemical Letters

外文期刊名：中国化学快报（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2017_2018】；

基金：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

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

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 heterocyclebased 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.
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 heterocyclebased 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.