Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β-Hydroxysteroid Dehydrogenase Type 1 (17 β-HSD1): The Role of the Bicyclic Moiety
Oster, Alexander, Klein, Tobias, Henn, Claudia, Werth, Ruth, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.
Published in ChemMedChem (07.03.2011)
Published in ChemMedChem (07.03.2011)
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Synthesis and Biological Evaluation of Phenyl Substituted 1H-1,2,4-Triazoles as Non-Steroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2
Al-Soud, Yaseen A., Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.
Published in Archiv der Pharmazie (Weinheim) (01.08.2012)
Published in Archiv der Pharmazie (Weinheim) (01.08.2012)
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17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog
Gargano, Emanuele M, Allegretta, Giuseppe, Perspicace, Enrico, Carotti, Angelo, Van Koppen, Chris, Frotscher, Martin, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W
Published in PloS one (31.07.2015)
Published in PloS one (31.07.2015)
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Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: conformationally restricted 17b-hydroxysteroid dehydrogenase type 2 (17b-HSD2) inhibitors
Perspicace, Enrico, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W
Published in Molecules (Basel, Switzerland) (16.04.2013)
Published in Molecules (Basel, Switzerland) (16.04.2013)
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Journal Article
Synthesis of Amidinohydrazones and Evaluation of Their Inhibitory Effect towards Aldosterone Synthase (CYP11B2) and the Formation of Selected Steroids
Voets, Marieke, Müller-Vieira, Ursula, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W.
Published in Archiv der Pharmazie (Weinheim) (01.07.2004)
Published in Archiv der Pharmazie (Weinheim) (01.07.2004)
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Journal Article
Mutational and structural studies uncover crucial amino acids determining activity and stability of 17β-HSD14
Badran, Mohammed J., Bertoletti, Nicole, Keils, Aline, Heine, Andreas, Klebe, Gerhard, Marchais-Oberwinkler, Sandrine
Published in The Journal of steroid biochemistry and molecular biology (01.05.2019)
Published in The Journal of steroid biochemistry and molecular biology (01.05.2019)
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Journal Article
Homology modeling meets site-directed mutagenesis: An ideal combination to elucidate the topology of 17β-HSD2
Sager, Christoph P., Weber, Susanne, Negri, Matthias, Banachowicz, Pauline, Möller, Gabriele, Adamski, Jerzy, Hartmann, Rolf W., Marchais-Oberwinkler, Sandrine
Published in The Journal of steroid biochemistry and molecular biology (01.02.2021)
Published in The Journal of steroid biochemistry and molecular biology (01.02.2021)
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17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development
Marchais-Oberwinkler, Sandrine, Henn, Claudia, Möller, Gabriele, Klein, Tobias, Negri, Matthias, Oster, Alexander, Spadaro, Alessandro, Werth, Ruth, Wetzel, Marie, Xu, Kuiying, Frotscher, Martin, Hartmann, Rolf W., Adamski, Jerzy
Published in The Journal of steroid biochemistry and molecular biology (01.05.2011)
Published in The Journal of steroid biochemistry and molecular biology (01.05.2011)
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Journal Article
Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors
Gargano, Emanuele Marco, Perspicace, Enrico, Carotti, Angelo, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W.
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
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Journal Article
New Insights into Human 17β-Hydroxysteroid Dehydrogenase Type 14: First Crystal Structures in Complex with a Steroidal Ligand and with a Potent Nonsteroidal Inhibitor
Bertoletti, Nicole, Braun, Florian, Lepage, Mahalia, Möller, Gabriele, Adamski, Jerzy, Heine, Andreas, Klebe, Gerhard, Marchais-Oberwinkler, Sandrine
Published in Journal of medicinal chemistry (28.07.2016)
Published in Journal of medicinal chemistry (28.07.2016)
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Journal Article
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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X-ray crystallography: essential tool for protein characterization and ligand optimization
Bertoletti, Nicole, Braun, Florian, Metz, Alexander, Heine, Andreas, Klebe, Gerhard, Marchais-Oberwinkler, Sandrine
Published in Acta crystallographica. Section A, Foundations and advances (01.12.2017)
Published in Acta crystallographica. Section A, Foundations and advances (01.12.2017)
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Journal Article
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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First Structure–Activity Relationship of 17β-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme
Braun, Florian, Bertoletti, Nicole, Möller, Gabriele, Adamski, Jerzy, Steinmetzer, Torsten, Salah, Mohamed, Abdelsamie, Ahmed S, van Koppen, Chris J, Heine, Andreas, Klebe, Gerhard, Marchais-Oberwinkler, Sandrine
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Journal Article
Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis
Abdelsamie, Ahmed S, Salah, Mohamed, Siebenbürger, Lorenz, Merabet, Ahmed, Scheuer, Claudia, Frotscher, Martin, Müller, Sebastian T, Zierau, Oliver, Vollmer, Günter, Menger, Michael D, Laschke, Matthias W, van Koppen, Chris J, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
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Journal Article
Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors with good ADME-related physicochemical parameters
Perspicace, Enrico, Giorgio, Annalaura, Carotti, Angelo, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W.
Published in European journal of medicinal chemistry (01.11.2013)
Published in European journal of medicinal chemistry (01.11.2013)
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Journal Article
Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy
Siebenbuerger, Lorenz, Hernandez-Olmos, Victor, Abdelsamie, Ahmed S, Frotscher, Martin, van Koppen, Chris J, Marchais-Oberwinkler, Sandrine, Scheuer, Claudia, Laschke, Matthias W, Menger, Michael D, Boerger, Carsten, Hartmann, Rolf W
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
New Drug-Like Hydroxyphenylnaphthol Steroidomimetics As Potent and Selective 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors for the Treatment of Estrogen-Dependent Diseases
Marchais-Oberwinkler, Sandrine, Wetzel, Marie, Ziegler, Erika, Kruchten, Patricia, Werth, Ruth, Henn, Claudia, Hartmann, Rolf W, Frotscher, Martin
Published in Journal of medicinal chemistry (27.01.2011)
Published in Journal of medicinal chemistry (27.01.2011)
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