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Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors
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
2013
DOI10.1002/ardp.201200267
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
WOS记录号WOS:000313692000006
引用统计
被引频次:9[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/400002259/52325
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Zhang, Xin.,Li, Ridong.,Qiao, Kang.,Ge, Zemei.,Zhang, Liangren.,...&Li, Runtao.(2013).Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors.ARCHIV DER PHARMAZIE,346(1),44-52.
MLA Zhang, Xin,et al."Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors".ARCHIV DER PHARMAZIE 346.1(2013):44-52.
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