title: Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.
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.
authors: Department of Chemistry, Scripps Florida, 5353 Parkside Drive, RE-2, Jupiter, FL 33458, USA.
authors: Joshua
authors: J
authors: Roth
authors: Franck
authors: F
authors: Madoux
authors: Peter
authors: P
authors: Hodder
authors: William R
authors: WR
authors: Roush
mesh_terms: D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054339:Steroidogenic Factor 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship; D017186:Titrimetry
chemical_list: D011804:Quinolines; D054339:Steroidogenic Factor 1; C037219:quinoline