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

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Miller CP, Bhaket P, Muthukaman N, Lyttle CR, Shomali M, Gallacher K, Slocum C, Hattersley G

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.

PubMed ID

21036041 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Metribolone	Androgen receptor	IC 50 (nM)	7	N/A	N/A	Details
Stanolone	Androgen receptor	IC 50 (nM)	10	N/A	N/A	Details
Testosterone	Androgen receptor	IC 50 (nM)	30	N/A	N/A	Details