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Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines
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
2011-06-15
DOI10.1016/j.bmcl.2011.04.096
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
WOS记录号WOS:000291145900027
项目编号20672009 ; 2009ZX09103-131
资助机构National Natural Science Foundation of China ; State Key New Drug Development Program
引用统计
被引频次:32[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61741
专题北京大学药学院
北京大学基础医学院
北京大学药学院_化学生物学系
作者单位Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
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.
APA Li, Ri-Dong,Zhang, Xin,Li, Qiao-Yan,Ge, Ze-Mei,&Li, Run-Tao.(2011).Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(12),3637-3640.
MLA Li, Ri-Dong,et al."Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.12(2011):3637-3640.
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