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学科主题: 药学
题名:
Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors
作者: Zhang, Xin1,2; Li, Ridong1; Qiao, Kang1; Ge, Zemei1; Zhang, Liangren1; Cheng, Tieming1; Li, Runtao1
关键词: Dithiocarbamic acid ester ; EGFR inhibitors ; Structure-activity relationship ; Synthesis
刊名: ARCHIV DER PHARMAZIE
发表日期: 2013
DOI: 10.1002/ardp.201200267
卷: 346, 期:1, 页:44-52
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: GROWTH-FACTOR RECEPTOR ; CANCER CHEMOPREVENTIVE ACTIVITY ; VITRO ANTITUMOR-ACTIVITY ; CELL LUNG-CANCER ; GEFITINIB ; KINASE ; DERIVATIVES ; MUTATIONS ; DESIGN ; BRASSININ
英文摘要:

Two series of dithiocarbamic acid esters, 4-anilinoquinazoline-6-ylmethylcarbamodithioic acid esters and 3-cyano-4-anilinoquinolin-6-ylmethylcarbamodithioic acid esters, were designed and synthesized. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay against three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Most of the compounds are equally or more potent than the positive control lapatinib. Three compounds (14d, 14h and 14i) were identified as dual inhibitors of the EGFR and ErbB-2 kinases and two compounds (14b and 14c) were identified as multi-target kinase inhibitors, and they are very worthy of further study. Installation of the dithiocarbamic acid ester group at the 6-position of 4-anilinoquinazoline or 3-cyano-4-anilinoquinoline could improve the inhibitory activity. Different dithiocarbamic acid ester groups significantly affect the activities.

语种: 英语
所属项目编号: 21172011 ; 2009ZX09103-131
项目资助者: National Natural Science Foundation of China ; State Key New Drug Development Program
WOS记录号: WOS:000313692000006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/52325
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.PLA, Gen Hosp, Affiliated Hosp 1, Dept Pharm, Beijing, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Zhang, Xin,Li, Ridong,Qiao, Kang,et al. Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors[J]. ARCHIV DER PHARMAZIE,2013,346(1):44-52.
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