New Insights into the SAR and Binding Modes of Bis(hydroxyphenyl)thiophenes and -benzenes: Influence of Additional Substituents on 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitory Activity and Selectivity
Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Negri, Matthias, Kruchten, Patricia, Oster, Alexander, Klein, Tobias, Spadaro, Alessandro, Werth, Ruth, Frotscher, Martin, Birk, Barbara, Hartmann, Rolf W
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Design, Synthesis, Biological Evaluation and Pharmacokinetics of Bis(hydroxyphenyl) substituted Azoles, Thiophenes, Benzenes, and Aza-Benzenes as Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)
Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Negri, Matthias, Al-Soud, Yaseen A, Kruchten, Patricia, Oster, Alexander, Frotscher, Martin, Birk, Barbara, Hartmann, Rolf W
Published in Journal of medicinal chemistry (13.11.2008)
Published in Journal of medicinal chemistry (13.11.2008)
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Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study
Abdelsamie, Ahmed S., van Koppen, Chris J., Bey, Emmanuel, Salah, Mohamed, Börger, Carsten, Siebenbürger, Lorenz, Laschke, Matthias W., Menger, Michael D., Frotscher, Martin
Published in European journal of medicinal chemistry (15.02.2017)
Published in European journal of medicinal chemistry (15.02.2017)
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Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme
Abdelsamie, Ahmed S., Bey, Emmanuel, Gargano, Emanuele M., van Koppen, Chris J., Empting, Martin, Frotscher, Martin
Published in European journal of medicinal chemistry (20.10.2015)
Published in European journal of medicinal chemistry (20.10.2015)
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Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker
Abdelsamie, Ahmed S., Bey, Emmanuel, Hanke, Nina, Empting, Martin, Hartmann, Rolf W., Frotscher, Martin
Published in European journal of medicinal chemistry (23.07.2014)
Published in European journal of medicinal chemistry (23.07.2014)
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Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases
Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Kruchten, Patricia, Frotscher, Martin, Werth, Ruth, Oster, Alexander, Algül, Oztekin, Neugebauer, Alexander, Hartmann, Rolf W.
Published in Bioorganic & medicinal chemistry (15.06.2008)
Published in Bioorganic & medicinal chemistry (15.06.2008)
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Journal Article
Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC 50 for a proof-of-principle study
Abdelsamie, Ahmed S, van Koppen, Chris J, Bey, Emmanuel, Salah, Mohamed, Börger, Carsten, Siebenbürger, Lorenz, Laschke, Matthias W, Menger, Michael D, Frotscher, Martin
Published in European journal of medicinal chemistry (15.02.2017)
Published in European journal of medicinal chemistry (15.02.2017)
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Journal Article
Novel estrone mimetics with high 17β-HSD1 inhibitory activity
Oster, Alexander, Klein, Tobias, Werth, Ruth, Kruchten, Patricia, Bey, Emmanuel, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.
Published in Bioorganic & medicinal chemistry (15.05.2010)
Published in Bioorganic & medicinal chemistry (15.05.2010)
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Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics
Marchais-Oberwinkler, Sandrine, Kruchten, Patricia, Frotscher, Martin, Ziegler, Erika, Neugebauer, Alexander, Bhoga, Umadevi, Bey, Emmanuel, Müller-Vieira, Ursula, Messinger, Josef, Thole, Hubert, Hartmann, Rolf W
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Selective inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17βHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells
Kruchten, Patricia, Werth, Ruth, Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.
Published in The Journal of steroid biochemistry and molecular biology (01.04.2009)
Published in The Journal of steroid biochemistry and molecular biology (01.04.2009)
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The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17β-Hydroxysteroid Dehydrogenase (17β-HSD) type 1 and type 2
Al-Soud, Yaseen A., Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Kruchten, Patricia, Frotscher, Martin, Hartmann, Rolf W.
Published in Molecular and cellular endocrinology (25.03.2009)
Published in Molecular and cellular endocrinology (25.03.2009)
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Journal Article
Development of biological assays for the identification of selective inhibitors of estradiol formation from estrone in rat liver preparations
Kruchten, Patricia, Werth, Ruth, Marchais-Oberwinkler, Sandrine, Bey, Emmanuel, Ziegler, Erika, Oster, Alexander, Frotscher, Martin, Hartmann, Rolf W.
Published in Comptes rendus. Chimie (01.10.2009)
Published in Comptes rendus. Chimie (01.10.2009)
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Journal Article
Aging Reduces the Efficacy of Estrogen Substitution to Attenuate Cardiac Hypertrophy in Female Spontaneously Hypertensive Rats
Jazbutyte, Virginija, Hu, Kai, Kruchten, Patricia, Bey, Emmanuel, Maier, Sebastian K.G, Fritzemeier, Karl-Heinrich, Prelle, Katja, Hegele-Hartung, Christa, Hartmann, Rolf W, Neyses, Ludwig, Ertl, Georg, Pelzer, Theo
Published in Hypertension (Dallas, Tex. 1979) (01.10.2006)
Published in Hypertension (Dallas, Tex. 1979) (01.10.2006)
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Journal Article
The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17beta-Hydroxysteroid Dehydrogenase (17beta-HSD) type 1 and type 2
Al-Soud, Yaseen A, Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Kruchten, Patricia, Frotscher, Martin, Hartmann, Rolf W
Published in Molecular and cellular endocrinology (25.03.2009)
Published in Molecular and cellular endocrinology (25.03.2009)
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Journal Article
Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17p-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases
BEY, Emmanuel, MARCHAIS-OBERWINKLER, Sandrine, KRUCHTEN, Patricia, FROTSCHER, Martin, WERTH, Ruth, OSTER, Alexander, ALGÜL, Oztekin, NEUGEBAUER, Alexander, HARTMANN, Rolf W
Published in Bioorganic & medicinal chemistry (2008)
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Published in Bioorganic & medicinal chemistry (2008)
Journal Article
Development of biological assays for the identification of selective inhibitors of estradiol formation from estrone in rat liver preparations: Méthodes physiques pour l'étude structurale de nouveaux matériaux
KRUCHTEN, Patricia, WERTH, Ruth, MARCHAIS-OBERWINKLER, Sandrine, BEY, Emmanuel, ZIEGLER, Erika, OSTER, Alexander, FROTSCHER, Martin, HARTMANN, Rolf W
Published in Comptes rendus. Chimie (2009)
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Published in Comptes rendus. Chimie (2009)
Journal Article
Novel estrone mimetics with high 17beta-HSD1 inhibitory activity
Oster, Alexander, Klein, Tobias, Werth, Ruth, Kruchten, Patricia, Bey, Emmanuel, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W
Published in Bioorganic & medicinal chemistry (15.05.2010)
Published in Bioorganic & medicinal chemistry (15.05.2010)
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Journal Article
Aging reduces the efficacy of estrogen substitution to attenuate cardiac hypertrophy in female spontaneously hypertensive rats. Commentary
HINOJOSA-LABORDE, Carmen, LINDSEY, Merry L, HARTMANN, Rolf W, NEYSES, Ludwig, ERTL, Georg, PELZER, Theo, JAZBUTYTE, Virginija, KAI HU, KRUCHTEN, Patricia, BEY, Emmanuel, MAIER, Sebastian K. G, FRITZEMEIER, Karl-Heinrich, PRELLE, Katja, HEGELE-HARTUNG, Christa
Published in Hypertension (Dallas, Tex. 1979) (2006)
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Published in Hypertension (Dallas, Tex. 1979) (2006)
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