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Items: 1 to 20 of 493

1.

Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.

Marchais-Oberwinkler S, Kruchten P, Frotscher M, Ziegler E, Neugebauer A, Bhoga U, Bey E, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.

J Med Chem. 2008 Aug 14;51(15):4685-98. doi: 10.1021/jm800367k. Epub 2008 Jul 17.

PMID:
18630892
2.

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.

Frotscher M, Ziegler E, Marchais-Oberwinkler S, Kruchten P, Neugebauer A, Fetzer L, Scherer C, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.

J Med Chem. 2008 Apr 10;51(7):2158-69. doi: 10.1021/jm701447v. Epub 2008 Mar 7.

PMID:
18324762
3.

Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).

Bey E, Marchais-Oberwinkler S, Werth R, Negri M, Al-Soud YA, Kruchten P, Oster A, Frotscher M, Birk B, Hartmann RW.

J Med Chem. 2008 Nov 13;51(21):6725-39. doi: 10.1021/jm8006917. Epub 2008 Oct 15.

PMID:
18855374
4.

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

Bey E, Marchais-Oberwinkler S, Kruchten P, Frotscher M, Werth R, Oster A, Algül O, Neugebauer A, Hartmann RW.

Bioorg Med Chem. 2008 Jun 15;16(12):6423-35. doi: 10.1016/j.bmc.2008.04.073. Epub 2008 May 3.

PMID:
18514529
5.

New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity.

Bey E, Marchais-Oberwinkler S, Negri M, Kruchten P, Oster A, Klein T, Spadaro A, Werth R, Frotscher M, Birk B, Hartmann RW.

J Med Chem. 2009 Nov 12;52(21):6724-43. doi: 10.1021/jm901195w.

PMID:
19831396
6.

New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.

Marchais-Oberwinkler S, Wetzel M, Ziegler E, Kruchten P, Werth R, Henn C, Hartmann RW, Frotscher M.

J Med Chem. 2011 Jan 27;54(2):534-47. doi: 10.1021/jm1009082. Epub 2010 Dec 28.

PMID:
21189020
7.

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.

Marchais-Oberwinkler S, Frotscher M, Ziegler E, Werth R, Kruchten P, Messinger J, Thole H, Hartmann RW.

Mol Cell Endocrinol. 2009 Mar 25;301(1-2):205-11. doi: 10.1016/j.mce.2008.09.024. Epub 2008 Oct 4.

PMID:
18950679
8.

Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1).

Spadaro A, Negri M, Marchais-Oberwinkler S, Bey E, Frotscher M.

PLoS One. 2012;7(1):e29252. doi: 10.1371/journal.pone.0029252. Epub 2012 Jan 5.

9.

Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.

Allan GM, Vicker N, Lawrence HR, Tutill HJ, Day JM, Huchet M, Ferrandis E, Reed MJ, Purohit A, Potter BV.

Bioorg Med Chem. 2008 Apr 15;16(8):4438-56. doi: 10.1016/j.bmc.2008.02.059. Epub 2008 Mar 7.

PMID:
18329273
10.

Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.

Lilienkampf A, Karkola S, Alho-Richmond S, Koskimies P, Johansson N, Huhtinen K, Vihko K, Wähälä K.

J Med Chem. 2009 Nov 12;52(21):6660-71. doi: 10.1021/jm900928k.

PMID:
19824648
11.
12.

Novel, potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.

Perspicace E, Cozzoli L, Gargano EM, Hanke N, Carotti A, Hartmann RW, Marchais-Oberwinkler S.

Eur J Med Chem. 2014 Aug 18;83:317-37. doi: 10.1016/j.ejmech.2014.06.036. Epub 2014 Jun 17.

PMID:
24974351
13.

Pharmacophore modelling of 17beta-HSD1 enzyme based on active inhibitors and enzyme structure.

Karkola S, Alho-Richmond S, Wahala K.

Mol Cell Endocrinol. 2009 Mar 25;301(1-2):225-8. doi: 10.1016/j.mce.2008.08.030. Epub 2008 Sep 6.

PMID:
18822344
14.

Estrone C15 derivatives--a new class of 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.

Messinger J, Husen B, Koskimies P, Hirvelä L, Kallio L, Saarenketo P, Thole H.

Mol Cell Endocrinol. 2009 Mar 25;301(1-2):216-24. doi: 10.1016/j.mce.2008.10.022. Epub 2008 Oct 25.

PMID:
19014997
15.

Development of a biological screening system for the evaluation of highly active and selective 17beta-HSD1-inhibitors as potential therapeutic agents.

Kruchten P, Werth R, Marchais-Oberwinkler S, Frotscher M, Hartmann RW.

Mol Cell Endocrinol. 2009 Mar 25;301(1-2):154-7. doi: 10.1016/j.mce.2008.09.035. Epub 2008 Oct 15.

PMID:
18984028
16.

Novel estrone mimetics with high 17beta-HSD1 inhibitory activity.

Oster A, Klein T, Werth R, Kruchten P, Bey E, Negri M, Marchais-Oberwinkler S, Frotscher M, Hartmann RW.

Bioorg Med Chem. 2010 May 15;18(10):3494-505. doi: 10.1016/j.bmc.2010.03.065. Epub 2010 Mar 29.

PMID:
20413314
17.

Synthesis and biological evaluation of (6- and 7-phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1.

Starcević S, Brozic P, Turk S, Cesar J, Rizner TL, Gobec S.

J Med Chem. 2011 Jan 13;54(1):248-61. doi: 10.1021/jm101104z. Epub 2010 Dec 7.

PMID:
21138273
18.

Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

Vicker N, Lawrence HR, Allan GM, Bubert C, Smith A, Tutill HJ, Purohit A, Day JM, Mahon MF, Reed MJ, Potter BV.

ChemMedChem. 2006 Apr;1(4):464-81.

PMID:
16892382
19.

Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

Allan GM, Lawrence HR, Cornet J, Bubert C, Fischer DS, Vicker N, Smith A, Tutill HJ, Purohit A, Day JM, Mahon MF, Reed MJ, Potter BV.

J Med Chem. 2006 Feb 23;49(4):1325-45.

PMID:
16480268

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