857153-47-0Relevant academic research and scientific papers
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
Zhang, Peilong,Dong, Jiaqiang,Zhong, Boyu,Zhang, Deyi,Jin, Can,Meng, Xuejing,Sun, Desheng,Xu, Xiangyuan,Zhou, Yong,Liang, Zhi,Ji, Minghua,Li, Hailong,Xu, Tao,Song, Guowei,Zhang, Ling,Chen, Gang,Yuan, Hongbin,Shih, Joe,Zhang, Ruihao,Hou, Guojun,Jin, Ying,Yang, Qiong
, p. 3738 - 3743 (2015)
Abstract A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model. Graphical abstract
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
