北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学药学院  > 化学生物学系  > 期刊论文
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

Files in This Item:

There are no files associated with this item.


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.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Zhang, Zhili]'s Articles
[Wu, Jun]'s Articles
[Ran, Fuxiang]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Zhang, Zhili]‘s Articles
[Wu, Jun]‘s Articles
[Ran, Fuxiang]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace