Inhibitors of protein kinase C. 1. 2, 3-Bisarylmaleimides

PD Davis, CH Hill, G Lawton, JS Nixon…

Index: Davis, Peter D.; Hill, Christopher H.; Lawton, Geoffrey; Nixon, John S.; Wilkinson, Sandra E.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 1 p. 177 - 184

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Citation Number: 207

Abstract

The design and synthesis of a series of novel inhibitors of protein kinase C (PKC) is described. These 2, 3-bisarylmaleimides were derived from the structural lead provided by the indolocarbazoles, staurosporine and K252a. Optimum activity required the imide NH, both carbonyl groups, and the olefinic bond of the maleimide ring. 2, 3-Bisindolylmaleimides were the most active, and the potency of these was improved by a chloro substituent at the ...