945557-08-4Relevant academic research and scientific papers
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids
Richardson, Timothy I.,Clarke, Christian A.,Yu, Kuo-Long,Yee, Ying K.,Bleisch, Thomas J.,Lopez, Jose E.,Jones, Scott A.,Hughes, Norman E.,Muehl, Brian S.,Lugar, Charles W.,Moore, Terry L.,Shetler, Pamela K.,Zink, Richard W.,Osborne, John J.,Montrose-Rafizadeh, Chahrzad,Patel, Nita,Geiser, Andrew G.,Galvin, Rachelle J. Sells,Dodge, Jeffrey A.
, p. 148 - 153 (2011)
We report the synthesis and characterization of novel 3-aryl indoles as potent and efficacious progesterone receptor (PR) antagonists with potential for the treatment of uterine fibroids. These compounds demonstrated excellent selectivity over other steroid nuclear hormone receptors such as the mineralocorticoid receptor (MR). They were prepared from 2-bromo-6-nitro indole in four to six steps using a Suzuki cross-coupling as the key step. Compound 8f was orally active in the complement 3 model of progesterone antagonism in the rat uterus and demonstrated partial antagonism in the McPhail model of progesterone activity.
INDOLE SULFONAMIDE MODULATORS OF PROGESTERONE RECEPTORS
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Page/Page column 47, (2008/06/13)
Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.
