Literature DB >> 17482463

Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.

Timothy I Richardson1, Scott A Frank, Minmin Wang, Christian A Clarke, Scott A Jones, Bai-Ping Ying, Dan T Kohlman, Owen B Wallace, Timothy A Shepherd, Robert D Dally, Alan D Palkowitz, Andrew G Geiser, Henry U Bryant, Judith W Henck, Ilene R Cohen, Daniel G Rudmann, Denis J McCann, David E Coutant, Samuel W Oldham, Conrad W Hummel, Kin C Fong, Ronald Hinklin, George Lewis, Hongqi Tian, Jeffrey A Dodge.   

Abstract

Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.

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Year:  2007        PMID: 17482463     DOI: 10.1016/j.bmcl.2007.04.044

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Parallel synthesis of a desketoraloxifene analogue library via iodocyclization/palladium-catalyzed coupling.

Authors:  Chul-Hee Cho; Dai-Il Jung; Benjamin Neuenswander; Richard C Larock
Journal:  ACS Comb Sci       Date:  2011-07-13       Impact factor: 3.784

2.  Consensus Induced Fit Docking (cIFD): methodology, validation, and application to the discovery of novel Crm1 inhibitors.

Authors:  Ori Kalid; Dora Toledo Warshaviak; Sharon Shechter; Woody Sherman; Sharon Shacham
Journal:  J Comput Aided Mol Des       Date:  2012-09-30       Impact factor: 3.686

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

Authors:  Timothy I Richardson; Christian A Clarke; Kuo-Long Yu; Ying K Yee; Thomas J Bleisch; Jose E Lopez; Scott A Jones; Norman E Hughes; Brian S Muehl; Charles W Lugar; Terry L Moore; Pamela K Shetler; Richard W Zink; John J Osborne; Chahrzad Montrose-Rafizadeh; Nita Patel; Andrew G Geiser; Rachelle J Sells Galvin; Jeffrey A Dodge
Journal:  ACS Med Chem Lett       Date:  2010-12-09       Impact factor: 4.345

4.  Innovative oral treatments of uterine leiomyoma.

Authors:  Mohamed Sabry; Ayman Al-Hendy
Journal:  Obstet Gynecol Int       Date:  2012-02-16
  4 in total

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