Inhibitors of protein kinase C. 1. 2, 3-Bisarylmaleimides
PD Davis, CH Hill, G Lawton, JS Nixon…
文献索引: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
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 ...