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学科主题: 药学
题名:
Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines
作者: Li, Ri-Dong; Zhang, Xin; Li, Qiao-Yan; Ge, Ze-Mei; Li, Run-Tao
关键词: Combination strategy ; Dithiocarbamic acid ester ; 4-Anilinoquinazoline ; EGFR inhibitor ; Synthesis
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2011-06-15
DOI: 10.1016/j.bmcl.2011.04.096
卷: 21, 期:12, 页:3637-3640
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: GROWTH-FACTOR RECEPTOR ; CELL LUNG-CANCER ; TYROSINE KINASE INHIBITION ; ANTITUMOR-ACTIVITY ; IN-VITRO ; MUTATIONS ; DESIGN ; AGENTS ; TUMOR
英文摘要:

On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of dithiocarbamic acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 20672009 ; 2009ZX09103-131
项目资助者: National Natural Science Foundation of China ; State Key New Drug Development Program
WOS记录号: WOS:000291145900027
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61741
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China

Recommended Citation:
Li, Ri-Dong,Zhang, Xin,Li, Qiao-Yan,et al. Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(12):3637-3640.
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