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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Predicting Putative Inhibitors of 17β-HSD1
Heinzerling, Lennart, Hartmann, Rolf W., Frotscher , Martin, Neumann , Dirk
Published in Molecular informatics (11.10.2010)
Published in Molecular informatics (11.10.2010)
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First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases
Salah, Mohamed, Abdelsamie, Ahmed S, Frotscher, Martin
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis
Mohamed, Abdelrahman, Salah, Mohamed, Tahoun, Mariam, Hawner, Manuel, Abdelsamie, Ahmed S., Frotscher, Martin
Published in Journal of medicinal chemistry (08.09.2022)
Published in Journal of medicinal chemistry (08.09.2022)
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Optimization of Hydroxybenzothiazoles as Novel Potent and Selective Inhibitors of 17β-HSD1
Spadaro, Alessandro, Frotscher, Martin, Hartmann, Rolf W
Published in Journal of medicinal chemistry (08.03.2012)
Published in Journal of medicinal chemistry (08.03.2012)
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A Hybrid In Silico/In Vitro Target Fishing Study to Mine Novel Targets of Urolithin A and B: A Step Towards a Better Comprehension of Their Estrogenicity
Dellafiora, Luca, Milioli, Marco, Falco, Angela, Interlandi, Margherita, Mohamed, Abdelrahman, Frotscher, Martin, Riccardi, Benedetta, Puccini, Paola, Rio, Daniele Del, Galaverna, Gianni, Dall'Asta, Chiara
Published in Molecular nutrition & food research (01.08.2020)
Published in Molecular nutrition & food research (01.08.2020)
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Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for In Vivo Proof-of-Principle Studies in an Endometriosis Mouse Model
Salah, Mohamed, Tahoun, Mariam, Rudzitis-Auth, Jeannette, Stotz, Lisa, van Koppen, Chris J., Laschke, Matthias W., Abdelsamie, Ahmed S., Frotscher, Martin
Published in Journal of medicinal chemistry (13.07.2023)
Published in Journal of medicinal chemistry (13.07.2023)
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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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Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17β-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation
Abdelsamie, Ahmed S., Salah, Mohamed, Siebenbürger, Lorenz, Hamed, Mostafa M., Börger, Carsten, van Koppen, Chris J., Frotscher, Martin, Hartmann, Rolf W.
Published in European journal of medicinal chemistry (15.09.2019)
Published in European journal of medicinal chemistry (15.09.2019)
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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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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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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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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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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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Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing
Abdelsamie, Ahmed S, Herath, Steven, Biskupek, Yannik, Börger, Carsten, Siebenbürger, Lorenz, Salah, Mohamed, Scheuer, Claudia, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Pohlemann, Tim, Menger, Michael D, Hartmann, Rolf W, Laschke, Matthias W, van Koppen, Chris J
Published in Journal of medicinal chemistry (14.02.2019)
Published in Journal of medicinal chemistry (14.02.2019)
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Bicyclic Substituted Hydroxyphenylmethanones as Novel Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) for the Treatment of Estrogen-Dependent Diseases
Oster, Alexander, Hinsberger, Stefan, Werth, Ruth, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W
Published in Journal of medicinal chemistry (25.11.2010)
Published in Journal of medicinal chemistry (25.11.2010)
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