Ontology highlight
ABSTRACT:
SUBMITTER: Whitby RJ
PROVIDER: S-EPMC4151520 | biostudies-literature | 2011 Apr
REPOSITORIES: biostudies-literature
Whitby Richard J RJ Stec Jozef J Blind Raymond D RD Dixon Sally S Leesnitzer Lisa M LM Orband-Miller Lisa A LA Williams Shawn P SP Willson Timothy M TM Xu Robert R Zuercher William J WJ Cai Fang F Ingraham Holly A HA
Journal of medicinal chemistry 20110310 7
The crystal structure of LRH-1 ligand binding domain bound to our previously reported agonist 3-(E-oct-4-en-4-yl)-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene 5 is described. Two new classes of agonists in which the bridgehead anilino group from our first series was replaced with an alkoxy or 1-ethenyl group were designed, synthesized, and tested for activity in a peptide recruitment assay. Both new classes gave very active compounds, particularly against SF-1. Structure-activity studies l ...[more]