Benzothiophene inhibitors of MK2. Part 1: Structure–activity relationships, assessments of selectivity and cellular potency

Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure–activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are presented. Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors.

The synthesis of a novel class of MK2 inhibitors is reported.Figure optionsDownload as PowerPoint slide