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学科主题: 药学
题名:
Synthesis and Bioactivity of N-5-Substituted 4-Amino-N-8,N-10-deazatetrahydrofolate Analogues
作者: 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
发表日期: 2011-11-01
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61465
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: Peking Univ, Dept Biol Chem, Sch Pharmaceut Sci, Beijing 100191, Peoples R China

Recommended Citation:
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.
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