17765-60-5Relevant academic research and scientific papers
Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators
Zhang, Xuqing,Li, Xiaojie,Allan, George F.,Sbriscia, Tifanie,Linton, Olivia,Lundeen, Scott G.,Sui, Zhihua
, p. 3857 - 3869 (2008/02/10)
A novel series of pyrazolines 2 have been designed, synthesized, and evaluated by in vivo screening as tissue-selective androgen receptor modulators (SARMs). Structure-activity relationships (SAR) were investigated at the R 1 to R6 positions as well as the core pyrazoline ring and the anilide linker. Overall, strong electron-withdrawing groups at the R 1 and R2 positions and a small group at the R5 and R6 position are optimal for AR agonist activity. The (S)-isomer of 7c exhibits more potent AR agonist activity than the corresponding (R)-isomer. (S)-7c exhibited an overall partial androgenic effect but full anabolic effect via oral administration in castrated rats. It demonstrated a noticeable antiandrogenic effect on prostate in intact rats with endogenous testosterone. Thus, (S)-7c is a tissue-selective nonsteroidal androgen receptor modulator with agonist activity on muscle and mixed agonist and antagonist activity on prostate.
Cinnamide and hydrocinnamide derivatives with kinase inhibitory activity
-
Page/Page column 178, (2008/06/13)
The present invention provides novel cinnamide compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
NOVEL HETEROCYCLE DERIVATIVES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS)
-
Page/Page column 78, (2008/06/13)
The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
