M. Frotscher

发表

Inhibitors of 17β-hydroxysteroid dehydrogenase type 1, 2 and 14: Structures, biological activities and future challenges

Mohamed Salah, Ahmed S. Abdelsamie, M. Frotscher, 2019, Molecular and Cellular Endocrinology.

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

R. Hartmann, M. Frotscher, Emmanuel Bey, 2008, Bioorganic & medicinal chemistry.

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.

Mohamed Salah, Ahmed S. Abdelsamie, M. Frotscher, 2017, Journal of medicinal chemistry.

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

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2009, Molecular and Cellular Endocrinology.

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 Salah, Ahmed S. Abdelsamie, M. Frotscher, 2022, 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.

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2011, Journal of medicinal chemistry.

Structure-based design and profiling of novel 17 beta-HSD14 inhibitors.

G. Klebe, A. Heine, J. Adamski, 2018 .

6‐Hydroxybenzothiophene Ketones: Potent Inhibitors of 17β‐Hydroxysteroid Dehydrogenase Type 1 (17β‐HSD1) Owing to Favorable Molecule Geometry and Conformational Preorganization

R. Hartmann, M. Engel, M. Frotscher, 2014, ChemMedChem.

Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.

R. Hartmann, M. Menger, G. Vollmer, 2019, Journal of medicinal chemistry.

Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)

Matthias Negri, M. Negri, M. Frotscher, 2012, PloS one.

1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.

R. Hartmann, M. Frotscher, G. Dannhardt, 2000, Journal of medicinal chemistry.

Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

R. Hartmann, C. Scherer, M. Frotscher, 2008, Journal of medicinal chemistry.

Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).

M. Negri, R. Hartmann, M. Frotscher, 2008, Journal of medicinal chemistry.

Synthesis, anti-17β-HSD and antiproliferative activity of new substituted 5-nitrosopyrimidine analogs

M. Frotscher, N. Al-Masoudi, N. A. Abdul-Rida, 2017, Medicinal Chemistry Research.

Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17β-HSD1.

R. Hartmann, M. Frotscher, A. Spadaro, 2012, Journal of medicinal chemistry.

Lead optimization of 17β-HSD1 inhibitors of the (hydroxyphenyl)naphthol sulfonamide type for the treatment of endometriosis.

R. Hartmann, A. Einspanier, M. Frotscher, 2012, Journal of medicinal chemistry.

Metabolism of endobiotics and therapeutic aspects of P450 inhibitors

R. Hartmann, M. Frotscher, G. Grün, 1997 .

17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development

M. Negri, R. Hartmann, J. Adamski, 2011, The Journal of Steroid Biochemistry and Molecular Biology.

Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.

R. Hartmann, M. Frotscher, Emmanuel Bey, 2008, Journal of medicinal chemistry.

New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity.

M. Negri, R. Hartmann, M. Frotscher, 2009, Journal of medicinal chemistry.

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.

M. Menger, M. Laschke, Mohamed Salah, 2017, European journal of medicinal chemistry.

Novel estrone mimetics with high 17beta-HSD1 inhibitory activity.

M. Negri, R. Hartmann, M. Frotscher, 2010, Bioorganic & medicinal chemistry.

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

R. Hartmann, M. Frotscher, Emmanuel Bey, 2009, The Journal of Steroid Biochemistry and Molecular Biology.

Novel Highly Active Thromboxane A2 Synthase Inhibitors Devoid of Carboxylic Groups

R. Hartmann, M. Frotscher, D. Ledergerber, 1997 .

Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2010, Journal of medicinal chemistry.

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

R. Hartmann, M. Frotscher, Emmanuel Bey, 2009, Molecular and Cellular Endocrinology.

Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.

R. Hartmann, M. Menger, T. Pohlemann, 2019, Journal of medicinal chemistry.

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.

R. Hartmann, M. Hamed, Mohamed Salah, 2019, European journal of medicinal chemistry.

17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog

R. Hartmann, Enrico Perspicace, A. Carotti, 2015, PloS one.

Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy.

R. Hartmann, M. Menger, M. Laschke, 2018, Journal of medicinal chemistry.

Synthesis and Biological Evaluation of Phenyl Substituted 1H‐1,2,4‐Triazoles as Non‐Steroidal Inhibitors of 17β‐Hydroxysteroid Dehydrogenase Type 2

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2012, Archiv der Pharmazie.

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

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2009, Molecular and Cellular Endocrinology.

Synthesis and Evaluation of Azole‐Substituted Tetrahydronaphthalenes as Inhibitors of P450 arom, P450 17, and P450 TxA2

R. Hartmann, M. Frotscher, G. Grün, 1996, Archiv der Pharmazie.

17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.

P. Jagodziński, R. Hartmann, G. Mangiatordi, 2021, ACS medicinal chemistry letters.

Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β‐Hydroxysteroid Dehydrogenase Type 1 (17 β‐HSD1): The Role of the Bicyclic Moiety

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2011, ChemMedChem.

Structural Basis for Species Specific Inhibition of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Computational Study and Biological Validation

M. Negri, M. Frotscher, T. Klein, 2011, PloS one.

Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker.

R. Hartmann, Ahmed S. Abdelsamie, M. Frotscher, 2014, European journal of medicinal chemistry.

Direct antiproliferative effect of nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 inhibitors in vitro

R. Hartmann, I. Zupkó, M. Frotscher, 2013, Journal of enzyme inhibition and medicinal chemistry.

Synthesis and Biological Evaluation of Phenyl Substituted 1H‐1,2,4‐Triazoles as Non‐Steroidal Inhibitors of 17β‐Hydroxysteroid Dehydrogenase Type 2.

R. Hartmann, M. Frotscher, S. Marchais-Oberwinkler, 2012 .

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.

G. Galaverna, C. Dall’Asta, Luca Dellafiora, 2020, Molecular nutrition & food research.

Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.

Ahmed S. Abdelsamie, M. Frotscher, Emmanuel Bey, 2015, European journal of medicinal chemistry.

Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids.

R. Hartmann, C. Scherer, K. Biemel, 2006, Journal of medicinal chemistry.

Development of biological assays for the identification of selective inhibitors of estradiol formation from estrone in rat liver preparations

R. Hartmann, M. Frotscher, Emmanuel Bey, 2009 .