4-Phenylpyrrolo [3, 4-c] carbazole-1, 3 (2 H, 6 H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and …

…, AM Thompson, RJ Booth, EM Dobrusin…

Index: Palmer, Brian D.; Thompson, Andrew M.; Booth, R. John; Dobrusin, Ellen M.; Kraker, Alan J.; Lee, Ho H.; Lunney, Elizabeth A.; Mitchell, Lorna H.; Ortwine, Daniel F.; Smaill, Jeff B.; Swan, Leesa M.; Denny, William A. Journal of Medicinal Chemistry, 2006 , vol. 49, # 16 p. 4896 - 4911

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Citation Number: 69

Abstract

High-throughput screening has identified a novel class of inhibitors of the checkpoint kinase Wee1, which have potential for use in cancer chemotherapy. These inhibitors are based on a 4-phenylpyrrolo [3, 4-c] carbazole-1, 3 (2 H, 6 H)-dione template and have been shown by X-ray crystallography to bind at the ATP site of the enzyme. An extensive study of the effects of substitution around this template has been carried out, which has identified substituents ...