Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors

…, S Nukui, J Lou, S Johnson, S Scales, I Botrous…

Index: Li, Hui; Hong, Yufeng; Nukui, Seiji; Lou, Jihong; Johnson, Sarah; Scales, Stephanie; Botrous, Iriny; Tompkins, Eileen; Yin, Chunfeng; Zhou, Ru; He, Mingying; Jensen, Jordan; Bouzida, Djamal; Alton, Gordon; Lafontaine, Jennifer; Grant, Stephan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 584 - 587

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Citation Number: 8

Abstract

A novel series of pyrrolopyrazole-based protein kinase C β 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.