Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids

TI Richardson, CA Clarke, KL Yu, YK Yee…

Index: 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. ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 2 p. 148 - 153

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Citation Number: 14

Abstract

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. ...