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学科主题: 药学
题名:
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: Design, synthesis and antifolate activity
作者: Zhang, Zhili1; Wu, Jun2; Ran, Fuxiang2; Guo, Ying1; Tian, Ran2; Zhou, Shouxin1; Wang, Xiaowei1; Liu, Zhenming2; Zhang, Liangren2; Cui, Jingrong2; Liu, Junyi1
关键词: Catalytic reduction ; Potential antitumor agents ; Folate derivatives ; Molecular modeling
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2009-02-01
DOI: 10.1016/j.ejmech.2008.04.017
卷: 44, 期:2, 页:764-771
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]: 5,10-DIDEAZA-5,6,7,8-TETRAHYDROFOLIC ACID DDATHF ; COLLAGEN-INDUCED ARTHRITIS ; BIOLOGICAL EVALUATION ; THYMIDYLATE SYNTHASE ; ANTITUMOR AGENTS ; FOLIC-ACID ; RHEUMATOID-ARTHRITIS ; 8-DEAZAFOLIC ACID ; ANALOGS ; METHOTREXATE
英文摘要:

We report, for the first time, the synthesis and biological activities of 8-deaza-5,6,7,8-tetrahydroaminopterin 9, and the 5-substituted and 5,10-disubstituted analogues 11, 13, 15, and 17. The analogues were obtained from key compound diethyl 8-deaza-5,6,7,8-tetrahydroaminopterin 8 following the catalytic reduction of the pyridine ring of diethyl 8-deaza aminopterin 5. The five novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives were assayed in vitro for their cytotoxicity on BGC-823, HL-60, Bel-7402 and Hela tumor cell lines, and inhibition on recombinant human dihydrofolate reductase (DHFR), among which the most potent molecule (compound 9) was about 4- to 10-fold poorer than MTX on the four kinds of tumor cell lines, and its effect on DHFR was about 17-fold poorer than MTX. The docking studies were followed to explain the biological testing results. (c) 2008 Elsevier Masson SAS. All rights reserved.

语种: 英语
项目资助者: Ministry of Education of China
WOS记录号: WOS:000264407800034
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56252
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 Biol Chem, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Zhang, Zhili,Wu, Jun,Ran, Fuxiang,et al. Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: Design, synthesis and antifolate activity[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2009,44(2):764-771.
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