Synthesis of 11β-(4-dimethylaminophenyl)-17β-hydroxy-17α-(3-methyl-1-butynyl)-4,9-estradien-3-one and 11β-(4-acetophenyl)-17β-hydroxy-17α-(3-methyl-1-butynyl)-4,9-estradien-3-one: two new analogs of mifepristone (RU-486)

Hazra, Braja G. ; Basu, Sourav ; Pore, Vandana S. ; Joshi, Padmakar L. ; Pal, Debnath ; Chakrabarti, Pinak (2000) Synthesis of 11β-(4-dimethylaminophenyl)-17β-hydroxy-17α-(3-methyl-1-butynyl)-4,9-estradien-3-one and 11β-(4-acetophenyl)-17β-hydroxy-17α-(3-methyl-1-butynyl)-4,9-estradien-3-one: two new analogs of mifepristone (RU-486) Steroids, 65 (3). pp. 157-162. ISSN 0039-128X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/S0039-128X(99)00097-5

Abstract

From the structure activity relationship, two new analogs, 2 and 3, of the potent progesterone antagonist mifepristone 1 have been designed. The syntheses of these two analogs have been achieved in eleven steps through modified synthetic sequences and improved procedures starting from (+)-estrone. In comparison with mifepristone 1, the relative binding affinities of compound 2 for the progesterone receptor was found to be more, whereas that of compound 3 was less.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Mifepristone Analogs; Progesterone Antagonist; Abortifacient; Antiglucocorticoid; Antiprogestin; 19-Norsteroids
ID Code:89225
Deposited On:24 Apr 2012 12:37
Last Modified:24 Apr 2012 12:37

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