Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
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DOI：
10.1016/j.bmcl.2015.06.021
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发表时间：
2015-09
影响因子：
2.7
通讯作者：
Peilong Zhang;Jiaqiang Dong;B. Zhong;D. Zhang;C. Jin;Xuejing Meng;Desheng Sun;Xiangyuan Xu;Yong Zhou;Zhipeng Liang;Minghua Ji;Hailong Li;Tao Xu;Guowei Song;Ling Zhang;Gang-Ying Chen;Hongbin Yuan;J. Shih;Ruihao Zhang;Guojun Hou;Ying-ying Jin;Qiong Yang
中科院分区：
文献类型：
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作者：
Peilong Zhang;Jiaqiang Dong;B. Zhong;D. Zhang;C. Jin;Xuejing Meng;Desheng Sun;Xiangyuan Xu;Yong Zhou;Zhipeng Liang;Minghua Ji;Hailong Li;Tao Xu;Guowei Song;Ling Zhang;Gang-Ying Chen;Hongbin Yuan;J. Shih;Ruihao Zhang;Guojun Hou;Ying-ying Jin;Qiong Yang
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,29ashowed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model.
