Synthesis of Small Molecule Inhibitors of the Orphan Nuclear Receptor Steroidogenic Factor-1 (NR5A1) Based on Isoquinolinone Scaffolds

摘要

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.