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

ChemMedChem, 2011-03, Vol.6 (3), p.476-487

2011

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Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1)

PloS one, 2012, Vol.7 (1), p.e29252-e29252

2012

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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

Archiv der Pharmazie (Weinheim), 2012-08, Vol.345 (8), p.610-621

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

PloS one, 2015-07, Vol.10 (7), p.e0134754-e0134754

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

Molecules (Basel, Switzerland), 2013-04, Vol.18 (4), p.4487-4509

2013

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Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)

Letters in drug design & discovery, 2011-06, Vol.8 (5), p.406-421

2011

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Mutational and structural studies uncover crucial amino acids determining activity and stability of 17β-HSD14

The Journal of steroid biochemistry and molecular biology, 2019-05, Vol.189, p.135-144

2019

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Homology modeling meets site-directed mutagenesis: An ideal combination to elucidate the topology of 17β-HSD2

The Journal of steroid biochemistry and molecular biology, 2021-02, Vol.206, p.105790, Article 105790

2021

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

The Journal of steroid biochemistry and molecular biology, 2011-05, Vol.125 (1), p.66-82

2011

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Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (1), p.21-24

2016

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Synthesis and Evaluation of Imidazolylmethylenetetrahydronaphthalenes and Imidazolylmethyleneindanes: Potent Inhibitors of Aldosterone Synthase

Journal of medicinal chemistry, 2005-03, Vol.48 (6), p.1796-1805

2005

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New Insights into Human 17β-Hydroxysteroid Dehydrogenase Type 14: First Crystal Structures in Complex with a Steroidal Ligand and with a Potent Nonsteroidal Inhibitor

Journal of medicinal chemistry, 2016-07, Vol.59 (14), p.6961-6967

2016

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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

Journal of medicinal chemistry, 2009-11, Vol.52 (21), p.6724-6743

2009

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17 beta -HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold

Bioorganic & medicinal chemistry, 2011-01, Vol.19 (2), p.807-815

2011

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X-ray crystallography: essential tool for protein characterization and ligand optimization

Acta crystallographica. Section A, Foundations and advances, 2017-12, Vol.73 (a2), p.C234-C234

2017

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First Structure–Activity Relationship of 17β-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme

Journal of medicinal chemistry, 2016-12, Vol.59 (23), p.10719-10737

2016

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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)

Journal of medicinal chemistry, 2008-11, Vol.51 (21), p.6725-6739

2008

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

Journal of medicinal chemistry, 2019-08, Vol.62 (15), p.7289-7301

2019

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Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors with good ADME-related physicochemical parameters

European journal of medicinal chemistry, 2013-11, Vol.69, p.201-215

2013

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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

Journal of medicinal chemistry, 2011-01, Vol.54 (2), p.534-547

2011

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

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10724-10738

2018

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

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1362-1372

2019

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Introduction of an Electron Withdrawing Group on the Hydroxyphenylnaphthol Scaffold Improves the Potency of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) Inhibitors

Journal of medicinal chemistry, 2011-11, Vol.54 (21), p.7547-7557

2011

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Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) Inhibitors

Molecules (Basel, Switzerland), 2013-04, Vol.18 (4), p.4487-4509

2013

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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

Journal of medicinal chemistry, 2010-11, Vol.53 (22), p.8176-8186

2010

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

Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1)

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

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

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

Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)

Mutational and structural studies uncover crucial amino acids determining activity and stability of 17β-HSD14

Homology modeling meets site-directed mutagenesis: An ideal combination to elucidate the topology of 17β-HSD2

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

Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors

Synthesis and Evaluation of Imidazolylmethylenetetrahydronaphthalenes and Imidazolylmethyleneindanes: Potent Inhibitors of Aldosterone Synthase

New Insights into Human 17β-Hydroxysteroid Dehydrogenase Type 14: First Crystal Structures in Complex with a Steroidal Ligand and with a Potent Nonsteroidal Inhibitor

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

17 beta -HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold

X-ray crystallography: essential tool for protein characterization and ligand optimization

First Structure–Activity Relationship of 17β-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme

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)

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

Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors with good ADME-related physicochemical parameters

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

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

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

Introduction of an Electron Withdrawing Group on the Hydroxyphenylnaphthol Scaffold Improves the Potency of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) Inhibitors

Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) Inhibitors

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

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