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Old 01-29-2016, 03:40 PM
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rss Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).

Related Articles Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).

ACS Med Chem Lett. 2016 Jan 14;7(1):83-8

Authors: Handlon AL, Schaller LT, Leesnitzer LM, Merrihew RV, Poole C, Ulrich JC, Wilson JW, Cadilla R, Turnbull P

Abstract
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 ?M), and high oral bioavailability in rats (83%).


PMID: 26819671 [PubMed]



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