Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors

A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38 alpha MAPK inhibitory activity (IC50 = 0.027 mu M), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells. (C) 2015 Elsevier Ltd. All rights reserved.