Potent, Nonsteroidal Selective Androgen Receptor Modulators (SARMs) Based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2007 Aug 21

PMID 17703938

Citations 1

Authors

Robert I Higuchi

Anthony W Thompson

Jyun-Hung Chen

Thomas R Caferro

Marquis L Cummings

Charlotte P Deckhut

Mark E Adams

Christopher M Tegley

James P Edwards

Francisco J Lopez

E Adam Kallel

Donald S Karanewsky

William T Schrader

Keith B Marschke

Lin Zhi

Affiliations

Soon will be listed here.

Abstract

A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar potency in vitro. Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10 mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action.

Citing Articles

Selective androgen receptor modulators in preclinical and clinical development.

Narayanan R, Mohler M, Bohl C, Miller D, Dalton J Nucl Recept Signal. 2008; 6:e010.

PMID: 19079612 PMC: 2602589. DOI: 10.1621/nrs.06010.

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