| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370569 | Bioorganic & Medicinal Chemistry Letters | 2015 | 6 Pages |
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.
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Related Topics
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Organic Chemistry
Authors
Peilong Zhang, Jiaqiang Dong, Boyu Zhong, Deyi Zhang, Can Jin, Xuejing Meng, Desheng Sun, Xiangyuan Xu, Yong Zhou, Zhi Liang, Minghua Ji, Hailong Li, Tao Xu, Guowei Song, Ling Zhang, Gang Chen, Hongbin Yuan, Joe Shih, Ruihao Zhang, Guojun Hou, Ying Jin,