Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.

Abdelhakim Hammach,Antonio Barbosa,Faith Corbo Gaenzler,Tazmeen Fadra,Daniel Goldberg,Ming-Hong Hao,Rachel R Kroe,Pingrong Liu,Kevin C Qian,Mark Ralph,Christopher Sarko,Fariba Soleymanzadeh,Neil Moss

Bioorganic & Medicinal Chemistry Letters（2007）

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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.

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关键词

p38 MAP kinase,Inhibitor,Benzimidazolone

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