Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds

J Roth, F Madoux, P Hodder, WR Roush

Index: Roth, Joshua; Madoux, Franck; Hodder, Peter; Roush, William R. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 8 p. 2628 - 2632

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Citation Number: 22

Abstract

Three synthetic routes were developed for structure–activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have improved potency, lower cellular toxicity, and improved selectivity compared to the initial HTS-derived leads 1 and 2.