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

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

Carsten Jagusch, Matthias Negri, Ulrike E. Hille, +11

Bioorganic & Medicinal Chemistry

Molecular PharmacologyHeterocyclic ModificationsPharmaceutical ChemistryBiochemistryCore Structure +10

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

Novel Aldosterone Synthase Inhibitors with Extended Carbocyclic Skeleton by a Combined Ligand-Based and Structure-Based Drug Design Approach

Simon Lucas, Ralf Heim, Matthias Negri, +6

Journal of Medicinal Chemistry

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

Ulrike E. Hille, Qingzhong Hu, Carsten A. Vock, +5

European Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryPharmaceutical ScienceDrug TargetBiochemistry +11

Synthesis, Biological Evaluation, and Molecular Modeling of Abiraterone Analogues: Novel CYP17 Inhibitors for the Treatment of Prostate Cancer

Mariano A. E. Pinto‐Bazurco Mendieta, Matthias Negri, Carsten Jagusch, +3

Journal of Medicinal Chemistry

Imidazolylmethylbenzophenones as Highly Potent Aromatase Inhibitors

Silvia Gobbi, Andrea Cavalli, Matthias Negri, +6

Journal of Medicinal Chemistry

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-<i>ij</i>]quinolin-4-one Derivatives

Simon Lucas, Matthias Negri, Ralf Heim, +2

Journal of Medicinal Chemistry

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

Qingzhong Hu, Matthias Negri, Kerstin Jahn‐Hoffmann, +6

Bioorganic & Medicinal Chemistry

Methylene ImidazoleMedicinal ChemistryBiochemistryMethylene BridgeBiocatalysis +8

Structure Optimization of 2-Benzamidobenzoic Acids as PqsD Inhibitors for Pseudomonas aeruginosa Infections and Elucidation of Binding Mode by SPR, STD NMR, and Molecular Docking

Elisabeth Weidel, Johannes C. de Jong, Christian Brengel, +7

Journal of Medicinal Chemistry

Pqsd InhibitorsStructure OptimizationAntimicrobial ChemotherapyChemical BiologyPharmaceutical Chemistry +16