Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase

…, KC Qian, M Ralph, C Sarko, F Soleymanzadeh…

文献索引：Hammach, Abdelhakim; Barbosa, Antonio; Gaenzler, Faith Corbo; Fadra, Tazmeen; Goldberg, Daniel; Hao, Ming-Hong; Kroe, Rachel R.; Liu, Pingrong; Qian, Kevin C.; Ralph, Mark; Sarko, Christopher; Soleymanzadeh, Fariba; Moss, Neil Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 24 p. 6316 - 6320

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被引用次数: 21

摘要

A new class of benzimidazolone p38 MAP kinase inhibitors was discovered through high- throughput screening. X-ray crystallographic data of the lead molecule with p38 were used to design analogues with improved binding affinity and potency in a cell assay of LPS- induced TNFα production. Herein, we report the SAR of this new class of p38 inhibitors.