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First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-¿B Activity As Novel Anticancer Agents.

Saarland University

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC

Saarland University

Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.

Saarland University

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

Saarland University

Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11ß-Hydroxylase.

Saarland University

Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.

Saarland University

Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.

Saarland University

Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4.

Saarland University

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

Saarland University

Novel, potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.

Saarland University

Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.

Saarland University

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

Saarland University

Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.

Saarland University

Structural optimization of 2,5-thiophene amides as highly potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors for the treatment of osteoporosis.

Saarland University

2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: development and prodrug concept.

Saarland University

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

Saarland University

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

Saarland University

Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.

Saarland University

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.

Saarland University

Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure.

Saarland University

Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA.

Saarland University

Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.

Saarland University

Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors for the treatment of osteoporosis.

Saarland University

Triazole ring-opening leads to the discovery of potent nonsteroidal 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.

Saarland University

Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors.

Saarland University

4-benzimidazolyl-3-phenylbutanoic acids as novel PIF-pocket-targeting allosteric inhibitors of protein kinase PKC¿.

Saarland University

Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.

Saarland University

New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.

Saarland University

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

Saarland University

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

Saarland University

Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.

Saarland University

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.

Saarland University

3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds.

Saarland University

Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls.

Saarland University

In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.

Saarland University

Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.

Saarland University

Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge.

Saarland University

Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.

Saarland University

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

Saarland University

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.

Saarland University

Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17.

Saarland University

Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for

Saarland University

Identification and Biochemical Characterization of Pyrrolidinediones as Novel Inhibitors of the Bacterial Enzyme MurA.

Saarland University

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

Saarland University

Metal-mediated inhibition of Escherichia coli methionine aminopeptidase: structure-activity relationships and development of a novel scoring function for metal-ligand interactions.

Saarland University

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.

Saarland University

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

Saarland University

Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.

Saarland University

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site.

Saarland University

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

Saarland University

Discovery and optimization of 1,3,5-trisubstituted pyrazolines as potent and highly selective allosteric inhibitors of protein kinase C-ζ.

Saarland University

Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors.

Saarland University

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.

Saarland University

Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.

Saarland University

Benzodiazepines as bromodomain inhibitors

Catalyst Therapeutics

Imidazo[1,2-α]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Arena Pharmaceuticals

Isoxazoline hydroxamic acid derivatives as LpxC inhibitors

Novartis

Triazine derivative and pharmaceutical composition having an analgesic activity comprising the same

Shionogi

Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases

Zhejiang Dtrm Biopharma

6-fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-quinazolin-4-one as an inhibitor of human phosphatidylinositol 3-kinase delta

Icos

Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase.

Universita Degli Studi Di Siena

Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.

Eli Lilly

4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.

Parke-Davis Pharmaceutical Research