Fragment-based discovery of novel phenyltriazolyl derivatives as allosteric type-I1/2 ALK inhibitors with promising antitumor effects
Bioorganic & Medicinal Chemistry Letters(2022)
摘要
•A series of phenyltriazolyl derivatives were developed as Type I1/2 ALK inhibitors.•12k exhibited promising inhibitory effects on ALKWT (3.7 nM) and ALKL1196M (6.8 nM).•12k induced apoptosis and inhibited colony formation & tumor migration on H2228 cells.•12k formed key interactions in ATP binding site and hydrophobic back pocket of ALK.
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关键词
Type-I1/2 ALK inhibitors,Phenyl-triazole,L1196M mutants,Antitumor,Computational analysis
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