Literature DB >> 17549597

Synthesis of C-11 modified mifepristone analog libraries.

Gregory L Hamilton1, Bradley J Backes.   

Abstract

Substitution of the C-11 aniline of mifepristone can provide compounds with altered pharmacokinetic and pharmacodynamic (PK/PD) profiles that may find use for new indications. The development of new steroid intermediates and specialized library synthesis methods were required to enable the efficient preparation of structurally complex C-11 modified mifepristone analogs.

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Year:  2007        PMID： 17549597     DOI： 10.1007/s11030-007-9058-4

Source DB:  PubMed          Journal:  Mol Divers        ISSN： 1381-1991            Impact factor:   2.943


  6 in total

1.  The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.

Authors:  Björn Kauppi; Clarissa Jakob; Mathias Färnegårdh; Jie Yang; Harri Ahola; Maria Alarcon; Karin Calles; Owe Engström; John Harlan; Steven Muchmore; Anna-Karin Ramqvist; Susanne Thorell; Lars Ohman; Jonathan Greer; Jan-Ake Gustafsson; Jan Carlstedt-Duke; Mats Carlquist
Journal:  J Biol Chem       Date:  2003-04-09       Impact factor: 5.157

Review 2.  Steroids and combinatorial chemistry.

Authors:  René Maltais; Martin R Tremblay; Liviu C Ciobanu; Donald Poirier
Journal:  J Comb Chem       Date:  2004 Jul-Aug

Review 3.  RU486 (mifepristone): mechanisms of action and clinical uses.

Authors:  F Cadepond; A Ulmann; E E Baulieu
Journal:  Annu Rev Med       Date:  1997       Impact factor: 13.739

4.  Regio and stereospecific synthesis of 11 beta-substituted 19-norsteroids. Influence of 11 beta-substitution on progesterone receptor affinity - (1).

Authors:  A Bélanger; D Philibert; G Teutsch
Journal:  Steroids       Date:  1981-04       Impact factor: 2.668

5.  Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.

Authors:  Thomas W von Geldern; Noah Tu; Philip R Kym; James T Link; Hwan-Soo Jae; Chunqiu Lai; Theresa Apelqvist; Patrik Rhonnstad; Lars Hagberg; Konrad Koehler; Marlena Grynfarb; Annika Goos-Nilsson; Johnny Sandberg; Marie Osterlund; Tomas Barkhem; Marie Höglund; Jiahong Wang; Steven Fung; Denise Wilcox; Phong Nguyen; Clarissa Jakob; Charles Hutchins; Mathias Färnegårdh; Björn Kauppi; Lars Ohman; Peer B Jacobson
Journal:  J Med Chem       Date:  2004-08-12       Impact factor: 7.446

6.  Pharmacokinetic properties of the antiglucocorticoid and antiprogesterone steroid RU 486 in man.

Authors:  S Kawai; L K Nieman; D D Brandon; R Udelsman; D L Loriaux; G P Chrousos
Journal:  J Pharmacol Exp Ther       Date:  1987-05       Impact factor: 4.030
  6 in total

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