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

Design, Synthesis, and Biological Evaluation of (Hydroxyphenyl)naphthalene and -quinoline Derivatives: Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) for the Treatment of Estrogen-Dependent Diseases

Martin Frotscher, Erika Ziegler, Sandrine Marchais‐Oberwinkler, +8

Journal of Medicinal Chemistry

Potent EstradiolPharmacotherapyPharmaceutical ChemistryGood SelectivityMolecular Pharmacology +15

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

Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics

Sandrine Marchais‐Oberwinkler, Patricia Kruchten, Martin Frotscher, +8

Journal of Medicinal Chemistry

1-Imidazolyl(alkyl)-Substituted Di- and Tetrahydroquinolines and Analogues:  Syntheses and Evaluation of Dual Inhibitors of Thromboxane A₂Synthase and Aromatase

Christoph Jacobs, Martin Frotscher, Gerd Dannhardt, +1

Journal of Medicinal Chemistry

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

Optimization of Hydroxybenzothiazoles as Novel Potent and Selective Inhibitors of 17β-HSD1

Alessandro Spadaro, Martin Frotscher, Rolf W. Hartmann

Journal of Medicinal Chemistry

Selective InhibitorsNovel PotentPharmacotherapyIntracellular Estradiol FormationPharmaceutical Chemistry +17

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