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Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents
Zhang, Zhili1; Tian, Chao1; Zhou, Shouxin1; Wang, Wei1; Guo, Ying1; Xia, Jie2; Liu, Zhenming2; Wang, Biao1; Wang, Xiaowei1; Golding, Bernard T.3; Griff, Roger J.3; Du, Yansheng4; Liu, Junyi1,2
关键词8-Deazatetrahydrofolates Antitumor Methionine synthase Folate inhibitor
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2012-12-01
DOI10.1016/j.ejmech.2012.09.027
58页:228-236
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]8-DEAZAFOLIC ACID ; ESCHERICHIA-COLI ; IN-VITRO ; INACTIVATION ; DERIVATIVES ; ANTIFOLATE ; ENZYMES ; ASSAY ; OXIDE
英文摘要

A number of 8-deazatetrahydrofolates bearing electrophilic groups on N-5 were designed and synthesized based on the action mechanism of methionine synthase, and their biological activities were investigated as well. Compounds (11b, 12b and 16) showed the most active against methionine synthase (IC50: 8.11 mu M, 1.73 mu M, 1.43 mu M). In addition, the cytotoxicity to human tumor cell lines and dihydrofolate reductase (DHFR) inhibition by target compounds were evaluated. (C) 2012 Elsevier Masson SAS. All rights reserved.

语种英语
WOS记录号WOS:000312745100022
引用统计
被引频次:10[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64877
专题北京大学药学院_化学生物学系
北京大学药学院
北京大学药学院_药物化学系
作者单位1.Peking Univ, Dept Chem Biol, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
3.Newcastle Univ, Dept Chem, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England
4.Indiana Univ Sch Med, Dept Neurol, Indianapolis, IN 46202 USA
推荐引用方式
GB/T 7714
Zhang, Zhili,Tian, Chao,Zhou, Shouxin,et al. Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,58:228-236.
APA Zhang, Zhili.,Tian, Chao.,Zhou, Shouxin.,Wang, Wei.,Guo, Ying.,...&Liu, Junyi.(2012).Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,58,228-236.
MLA Zhang, Zhili,et al."Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 58(2012):228-236.
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