Ontology highlight
ABSTRACT:
SUBMITTER: Handlon AL
PROVIDER: S-EPMC4716610 | biostudies-literature | 2016 Jan
REPOSITORIES: biostudies-literature
Handlon Anthony L AL Schaller Lee T LT Leesnitzer Lisa M LM Merrihew Raymond V RV Poole Chuck C Ulrich John C JC Wilson Joseph W JW Cadilla Rodolfo R Turnbull Philip P
ACS medicinal chemistry letters 20151119 1
A series of selective androgen receptor modulators (SARMs) containing the 1-(trifluoromethyl)benzyl alcohol core have been optimized for androgen receptor (AR) potency and drug-like properties. We have taken advantage of the lipophilic ligand efficiency (LLE) parameter as a guide to interpret the effect of structural changes on AR activity. Over the course of optimization efforts the LLE increased over 3 log units leading to a SARM 43 with nanomolar potency, good aqueous kinetic solubility (>700 ...[more]