Title of article :
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones
Author/Authors :
Robert I. Higuchi، نويسنده , , Anthony W. Thompson، نويسنده , , Jyun-Hung Chen، نويسنده , , Thomas R. Caferro، نويسنده , , Marquis L. Cummings، نويسنده , , Charlotte P. Deckhut، نويسنده , , Mark E. Adams، نويسنده , , Christopher M. Tegley، نويسنده , , James P. Edwards، نويسنده , , Francisco J. Lopez، نويسنده , , E. Adam Kallel، نويسنده , , Donald S. Karanewsky، نويسنده , , William T. Schrader، نويسنده , , Keith B. Marschke، نويسنده , , Lin Zhi، نويسنده ,
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.
Keywords :
Androgen , SARM , 3-f]quinolin-8-one , testosterone , Anabolic , AR , Androgenic , Benzoxazine
