| 18324762 |
Frotscher M, Ziegler E, Marchais-Oberwinkler S, Kruchten P, Neugebauer A, Fetzer L, Scherer C, Muller-Vieira U, Messinger J, Thole H, Hartmann RW: Design, synthesis, and biological evaluation of (hydroxyphenyl) naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases. J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7.
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85(1,1,1,5) |
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| 18950679 |
Marchais-Oberwinkler S, Frotscher M, Ziegler E, Werth R, Kruchten P, Messinger J, Thole H, Hartmann RW: Structure-activity study in the class of 6-(3'-hydroxyphenyl) naphthalenes leading to an optimization of a pharmacophore model for 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors. Mol Cell Endocrinol. 2009 Mar 25;301(1-2):205-11. Epub 2008 Oct 4.
After identification of the 6-(3'-hydroxyphenyl)-2-naphthol scaffold 1, the potency of this class of inhibitors was further improved by substitution of the 1-position of the naphthalene ring by a phenyl group (compound 18, IC (50)=20nM). |
3(0,0,0,3) |
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