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Synthesis and Bioactivity of 8-Deaza Folic Acid Analogues of Thiophene
Zhou Shouxin1; Tian Chao1; Guo Ying1; Wang Xiaowei1; Liu Junyi1,2; Zhang Zhili1
关键词Thiophene Derivatives Of 8-deaza Folic Acid Methionine Synthase Dihydrofolate Reductase Nitration Bioactivity
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
2012-10-01
DOI10.6023/cjoc1203122
32期:10页:1944-1950
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]ANTIFOLATE ; STRESS
英文摘要

Based on the action mechanism of methionine synthase and structures of inhibitors against dihydrofolic reductase, thiophene derivatives of 8-deaza folic acid were designed as dual-target inhibitors. Two target compounds were obtained by nitration, reduction, condensation, and hydrolysis with 2-thiophenecarboxylic acid as starting material, and were characterized by H-1 NMR, C-13 NMR and MS techniques. The inhibitory activities against methionine synthase and recombinant human dihydrofolate reductase were determined. The target compounds showed inhibitory activity on both two enzymes. The IC(50)s of one compound were 25.2 and 2.3 mu mol/L against methionine synthase and recombinant human dihydrofolate reductase, respectively.

语种中文
WOS记录号WOS:000311063800020
项目编号21042009 ; 21172014 ; 2009ZX09301-010
资助机构National Science Foundation of China ; Ministry of Science and Technology of China
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51848
专题北京大学药学院_化学生物学系
北京大学药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Zhou Shouxin,Tian Chao,Guo Ying,et al. Synthesis and Bioactivity of 8-Deaza Folic Acid Analogues of Thiophene[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2012,32(10):1944-1950.
APA Zhou Shouxin,Tian Chao,Guo Ying,Wang Xiaowei,Liu Junyi,&Zhang Zhili.(2012).Synthesis and Bioactivity of 8-Deaza Folic Acid Analogues of Thiophene.CHINESE JOURNAL OF ORGANIC CHEMISTRY,32(10),1944-1950.
MLA Zhou Shouxin,et al."Synthesis and Bioactivity of 8-Deaza Folic Acid Analogues of Thiophene".CHINESE JOURNAL OF ORGANIC CHEMISTRY 32.10(2012):1944-1950.
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