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Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis

文献类型：期刊论文

作者Wang, Qi11; Tang, Bixi5,8,9; Sun, Dandan4; Dong, Ying8,9; Ji, Yinchun3,10; Shi, Huanyu8,11; Zhou, Liwei6,7,11; Yang, Yueyue8,11; Luo, Menglan2,11; Tan, Qian9
刊名ACTA PHARMACEUTICA SINICA B
出版日期2022-04-01
卷号12期号:4页码:1943-1962
ISSN号2211-3835
关键词Idiopathic pulmonary fibrosis Discoidin domain receptor Kinase Inhibitor Docking
DOI10.1016/j.apsb.2021.11.012
通讯作者Xiong, Bing(bxiong@simm.ac.cn) ; Li, Jia(jli@simm.ac.cn) ; Chen, Danqi(dqchen@simm.ac.cn)
英文摘要Idiopathic pulmonary fibrosis (IPF) is a chronic fatal lung disease with a median survival time of 3e5 years. Inaccurate diagnosis, limited clinical therapy and high mortality together indicate that the development of effective therapeutics for IPF is an urgent need. In recent years, it was reported that DDRs are potential targets in anti-fibrosis treatment. Based on previous work we carried out further structure modifications and led to a more selective inhibitor 47 by averting some fibrosis-unrelated kinases, such as RET, AXL and ALK. Extensive profiling of compound 47 has demonstrated that it has potent DDR1/2 inhibitory activities, low toxicity, good pharmacokinetic properties and reliable in vivo anti fibrosis efficacy. Therefore, we confirmed that discoidin domain receptors are promising drug targets for IPF, and compound 47 would be a promising candidate for further drug development. (C) 2022 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
WOS关键词KINASE INHIBITORS ; TYROSINE KINASES ; OPTIMIZATION
资助项目Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020323] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China[2018ZX09711002-004-009] ; Strategic Priority Research Program of Chinese Academy of Sciences[SIMM010203] ; Institutes for Drug Discovery and Development, Chinese Academy of Sciences[CASIMM0120215009] ; National Natural Science Foundation of China[U1703235] ; Shanghai Science and Technology Development Funds (China)[18431907100]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
WOS记录号WOS:000808331500003
源URL[http://119.78.100.183/handle/2S10ELR8/301542]  
专题新药研究国家重点实验室
通讯作者Xiong, Bing; Li, Jia; Chen, Danqi
作者单位1.UCAS, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
2.Shanghai Univ, Dept Chem, Coll Sci, Shanghai 200444, Peoples R China
3.Fudan Univ, Shanghai Fifth Peoples Hosp, Dept Pulm & Crit Care Med, Shanghai 200240, Peoples R China
4.Nanjing Univ Chinese Med, Sch Chinese Mat Medica, Nanjing 210023, Peoples R China
5.Fudan Univ, Sch Pharm, Dept Pharmacol, Shanghai 201203, Peoples R China
6.Shanghai Univ, Coll Sci, Dept Chem, Shanghai 200444, Peoples R China
7.Shanghai Univ, Coll Sci, Ctr Supramol Chem & Catalysis, Shanghai 200444, Peoples R China
8.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
9.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
10.Chinese Acad Sci, Shanghai Inst Mat Med, Div Anti Tumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Qi,Tang, Bixi,Sun, Dandan,et al. Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis[J]. ACTA PHARMACEUTICA SINICA B,2022,12(4):1943-1962.
APA Wang, Qi.,Tang, Bixi.,Sun, Dandan.,Dong, Ying.,Ji, Yinchun.,...&Chen, Danqi.(2022).Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis.ACTA PHARMACEUTICA SINICA B,12(4),1943-1962.
MLA Wang, Qi,et al."Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis".ACTA PHARMACEUTICA SINICA B 12.4(2022):1943-1962.

入库方式： OAI收割

来源：上海药物研究所

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