原创力文档discovery of quinone-directed antitumor agents selectively bioactivated by nqo1 over cpr with improved safety profile：（发现quinone-directed抗肿瘤药物选择性地bioactivated nqo1在心肺复苏与改进的安全性）.pdfVIP
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discovery of quinone-directed antitumor agents selectively bioactivated by nqo1 over cpr with improved safety profile：（发现quinone-directed抗肿瘤药物选择性地bioactivated nqo1在心肺复苏与改进的安全性）
European Journal of Medicinal Chemistry 129 (2017) 27e40
Contents lists available at ScienceDirect
European Journal of Medicinal Chemistry
journal homepage: /locate/ejmech
Research paper
Discovery of quinone-directed antitumor agents selectively
bioactivated by NQO1 over CPR with improved safety profile
a, 1 a, 1 a a, b a, *
Jinlei Bian , Xiang Li , Nan Wang , Xingsen Wu , Qidong You ,
Xiaojin Zhang a, b, **
a State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009,
China
b Department of Organic Chemistry, School of Science, China Pharmaceutical University, Nanjing 210009, China
a r t i c l e i n f o a b s t r a c t
Article history: In this work, we mainly focused on discovering compounds with good selectivity for NQO1 over CPR. The
Received 25 November 2016 NQO1-mediated two-electron reduction of compounds would kill cancer cells selectively, while CPR-
Received in revised form mediated one-electron reduction would induce potential hepatotoxicity. Several novel quinone-
3 February 2017
directed antitumor agents were discovered as specific NQO1 substrates through structure-activity
Accepted 4 February 2017
relationship studies. Among them, compound 3,7,8-trimethylnaphtho[1,2-b]
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