Identification of novel pyrrolopyrazoles as protein kinase C beta II inhibitors

A novel series of pyrrolopyrazole-based protein kinase C beta II inhibitors has been identified from high-throughput screening. Herein, we report our initial structure-activity relationship studies with a focus on optimizing compound ligand efficiency and physicochemical properties, which has led to potent inhibitors with good cell permeability. (C) 2010 Elsevier Ltd. All rights reserved.