Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs)

Chris P Miller; Pushpal Bhaket; Nagarajan Muthukaman; C Richard Lyttle; Maysoun Shomali; Kyla Gallacher; Connie Slocum; Gary Hattersley

doi:10.1016/j.bmcl.2010.09.140

Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs)

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7516-20. doi: 10.1016/j.bmcl.2010.09.140. Epub 2010 Oct 7.

Authors

Chris P Miller¹, Pushpal Bhaket, Nagarajan Muthukaman, C Richard Lyttle, Maysoun Shomali, Kyla Gallacher, Connie Slocum, Gary Hattersley

Affiliation

¹ Radius Health, Inc., 300 Technology Square, Cambridge, MA 02139, USA. cmiller@radiuspharm.com

PMID: 21036041
DOI: 10.1016/j.bmcl.2010.09.140

Abstract

The synthesis and in vitro binding affinity for a novel series of potent androgen receptor modulators is described. One of the more potent compounds (17, RAD35010) was further characterized in vivo where it restored levator ani weight in castrated male rats to near sham level while having no significant effect on prostate weight.

MeSH terms

Administration, Oral
Animals
Carbazoles / chemical synthesis
Carbazoles / chemistry*
Carbazoles / pharmacology
Male
Prostate / drug effects
Rats
Receptors, Androgen / chemistry*
Receptors, Androgen / metabolism

Substances

Carbazoles
Receptors, Androgen