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ID: ALA3603807
Journal: Bioorg Med Chem Lett
Title: Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Authors: Zhang P, Dong J, Zhong B, Zhang D, Jin C, Meng X, Sun D, Xu X, Zhou Y, Liang Z, Ji M, Li H, Xu T, Song G, Zhang L, Chen G, Yuan H, Shih J, Zhang R, Hou G, Jin Y, Yang Q.
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.
CiteXplore: 26130408