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)

Emmanuel Bey, Sandrine Marchais‐Oberwinkler, Ruth Werth, +7

Journal of Medicinal Chemistry

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

Emmanuel Bey, Sandrine Marchais‐Oberwinkler, Matthias Negri, +8

Journal of Medicinal Chemistry

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

Emmanuel Bey, Sandrine Marchais‐Oberwinkler, Patricia Kruchten, +6

Bioorganic & Medicinal Chemistry

Medicinal ChemistryEstrogen-dependent DiseasesBiochemistryMedicineNatural Sciences +9

New Drug-Like Hydroxyphenylnaphthol Steroidomimetics As Potent and Selective 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors for the Treatment of Estrogen-Dependent Diseases

Sandrine Marchais‐Oberwinkler, Marie Wetzel, Erika Ziegler, +5

Journal of Medicinal Chemistry

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

Patricia Kruchten, Ruth Werth, Sandrine Marchais‐Oberwinkler, +2

Molecular and Cellular Endocrinology

Drug TargetBiological Screening SystemPotential Therapeutic AgentsBiochemistrySelective 17β-Hsd1-inhibitors +7

Selective inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17βHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells

Patricia Kruchten, Ruth Werth, Emmanuel Bey, +4

The Journal of Steroid Biochemistry and Molecular Biology

Selective InhibitionBreast OncologyResponsive Cell GrowthBreast CancerAromatase +6

Bicyclic Substituted Hydroxyphenylmethanones as Novel Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) for the Treatment of Estrogen-Dependent Diseases

Alexander Oster, Stefan Hinsberger, Ruth Werth, +3

Journal of Medicinal Chemistry

Chemoprevention StrategyBicyclic Substituted HydroxyphenylmethanonesChemical BiologyPharmaceutical ChemistryMolecular Pharmacology +17

Novel estrone mimetics with high 17β-HSD1 inhibitory activity

Alexander Oster, Tobias Klein, Ruth Werth, +6

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryNovel Estrone MimeticsMedicineNatural Sciences +5

Structure–activity study in the class of 6-(3′-hydroxyphenyl)naphthalenes leading to an optimization of a pharmacophore model for 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitors

Sandrine Marchais‐Oberwinkler, Martin Frotscher, Erika Ziegler, +5

Molecular and Cellular Endocrinology

Molecular PharmacologyMedicinal ChemistryDrug TargetBiochemistryMedicine +9

The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17β-Hydroxysteroid Dehydrogenase (17β-HSD) type 1 and type 2

Yaseen A. Al‐Soud, Emmanuel Bey, Alexander Oster, +5

Molecular and Cellular Endocrinology

Molecular PharmacologyMedicinal ChemistryType 1BiochemistryMedicine +6