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Synthesis and Bioactivity of N-5-Substituted 4-Amino-N-8,N-10-deazatetrahydrofolate Analogues
Tian Chao; Li Chao; Zhang Zhili; Wang Xiaowei; Liu Junyi
关键词4-amino-N-8,N-10-deazatetrahydrofolate analogue thymidylate synthetase anticancer activity
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
2011-11-01
31期:11页:1820-1827
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]THYMIDYLATE SYNTHASE ; STRUCTURAL MECHANISM ; CRYSTAL-STRUCTURE ; INHIBITORS ; DESIGN
英文摘要

The backbone of folate analogue was constructed via Wittig reaction between 2,4-diamino-6-hydroxymethylpyrido[3,2-d]pyrimidine and diethyl-N[4-(formyl)benzoyl]-L-glutamate. Four new 4-amino-N-8,N-10-deazatetrahydrofolate analogues were obtained by hydrogenating of pyridine ring and linking different substituent on N-5 position. The compounds were characterized by H-1 NMR, C-13 NMR and MS techniques. The inhibitory activities against human thymidylate synthetase were determined. The results showed that the bioactivities of the compounds were related with different substituents on N-5 position. The inhibitory rates of two compounds against leukemia cell line HL-60 were above 60% at 0.1 mu mol.L-1.

语种中文
WOS记录号WOS:000297908100009
引用统计
被引频次:2[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/400002259/61465
专题北京大学药学院_化学生物学系
作者单位Peking Univ, Dept Biol Chem, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Tian Chao,Li Chao,Zhang Zhili,et al. Synthesis and Bioactivity of N-5-Substituted 4-Amino-N-8,N-10-deazatetrahydrofolate Analogues[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2011,31(11):1820-1827.
APA Tian Chao,Li Chao,Zhang Zhili,Wang Xiaowei,&Liu Junyi.(2011).Synthesis and Bioactivity of N-5-Substituted 4-Amino-N-8,N-10-deazatetrahydrofolate Analogues.CHINESE JOURNAL OF ORGANIC CHEMISTRY,31(11),1820-1827.
MLA Tian Chao,et al."Synthesis and Bioactivity of N-5-Substituted 4-Amino-N-8,N-10-deazatetrahydrofolate Analogues".CHINESE JOURNAL OF ORGANIC CHEMISTRY 31.11(2011):1820-1827.
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