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ID: ALA1144830

Journal: Bioorg Med Chem Lett

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

Authors: Roth J, Madoux F, Hodder P, Roush WR.

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.

CiteXplore: 18374567

DOI: 10.1016/j.bmcl.2008.03.027