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Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors

文献类型：期刊论文

作者Fu, Yan1; Tang, Shuai2; Su, Yi2; Lan, Xiaojing2; Ye, Yan1; Zha, Chuantao1; Li, Lei1; Cao, Jianhua1; Chen, Yi2; Jiang, Lei1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2017-12-01
卷号27期号:23页码:5332-5336
关键词Cyclin-dependent kinase CDK inhibitor Structure-activity relationship In vitro and in vivo profiling
ISSN号0960-894X
DOI10.1016/j.bmcl.2017.09.050
文献子类Article
英文摘要The discovery of a class of diheteroaromatic amines based on LY2835219 as cyclin-dependent kinase (CDK1/4/6) inhibitors was described. The series was found to have much more improved CDK1 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. The synthesis and structure-activity relationship studies of these compounds were reported. One promising compound was selected to evaluate as a novel lead compound after in vitro and in vivo profiling. (C) 2017 Elsevier Ltd. All rights reserved.
WOS关键词CANCER ; PHASE-1 ; KINASE
资助项目Shanghai Science and Technology Committee, China[16431902600]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000415643400044
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/272381]  
专题药理学第一研究室
通讯作者Huang, Min; Wan, Huixin
作者单位1.Shanghai HaiHe Pharmaceutial Co Ltd, 421 Newton Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Fu, Yan,Tang, Shuai,Su, Yi,et al. Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(23):5332-5336.
APA Fu, Yan.,Tang, Shuai.,Su, Yi.,Lan, Xiaojing.,Ye, Yan.,...&Wan, Huixin.(2017).Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(23),5332-5336.
MLA Fu, Yan,et al."Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.23(2017):5332-5336.

入库方式： OAI收割

来源：上海药物研究所

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