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学科主题: 药学
题名:
Mechanism-based design, synthesis and biological studies of N-5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents
作者: 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
发表日期: 2012-12-01
DOI: 10.1016/j.ejmech.2012.09.027
卷: 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
所属项目编号: 20972011 ; 21042009 ; 21172014 ; 2009ZX09301-010
项目资助者: National Science Foundation of China ; Ministry of Science and Technology of China
WOS记录号: WOS:000312745100022
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64877
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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

Recommended Citation:
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.
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