852569-35-8Relevant articles and documents
The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening
Lanter, James C.,Fiordeliso, James J.,Jiang, Weiqin,Allan, George F.,Lai, Muh-Tsann,Linton, Olivia,Hahn, Do Won,Lundeen, Scott G.,Sui, Zhihua
, p. 123 - 126 (2007)
A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify compoun
A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
Lanter, James C.,Fiordeliso, James J.,Allan, George F.,Musto, Amy,Hahn, Do Won,Sui, Zhihua
, p. 5646 - 5649 (2007/10/03)
Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiety in the parent compound. Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain.
Novel indole derivatives as selective androgen receptor modulators (SARMS)
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Page/Page column 58, (2008/06/13)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.