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学科主题: 药学
题名:
Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives
作者: Deng Xiling1,3; Liu Weidong1; Li Chao1; Zhang Zhili1; Wang Xiaowei1; Liu Junyi1,2
关键词: 5-(substituted)amino pyrimidine ; new anticancer agent ; synthesis
刊名: CHINESE JOURNAL OF ORGANIC CHEMISTRY
发表日期: 2011
卷: 31, 期:1, 页:75-81
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
英文摘要:

A new practical approach to prepare diethyl N-{4-[N-methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]benzoyl}-L-glutamate and its derivatives has been realized from ethyl 4-aminobenzoate (4a) and diethyl N-(4-aminobenzoyl)-L-glutamate (4b). Six novel 5-(substituted)amino pyrimidines 9 similar to 11 were synthesized via methylation, allylation, bromohydroxylation, epoxidation, ring-opening, deprotection reaction and so on, and were characterized by (1)H NMR, (13)C NMR and MS techniques. The inhibitory activities against human dihydrofolate reductase of the compounds have been determined. The results showed that the bioactivities of the compounds were related with L-glutamate side chain.

语种: 中文
WOS记录号: WOS:000287782400008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50526
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, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drug, Beijing 100191, Peoples R China
3.Shihezi Univ, Sch Pharmaceut Sci, Dept Pharmaceut Sci, Shihezi 832002, Peoples R China

Recommended Citation:
Deng Xiling,Liu Weidong,Li Chao,et al. Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2011,31(1):75-81.
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