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

  • Bioorg Med Chem Lett. 2008 Apr 15;18(8):2628-32. doi: 10.1016/j.bmcl.2008.03.027.
Joshua Roth  1 ,  Franck Madoux ,  Peter Hodder ,  William R Roush
Affiliations
  • 1. Department of Chemistry, Scripps Florida, 5353 Parkside Drive, RE-2, Jupiter, FL 33458, USA.
PMID: 18374567 DOI: 10.1016/j.bmcl.2008.03.027
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.

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