Fluorine Interactions at the Thrombin Active Site: Protein Backbone Fragments HC_αCO Comprise a Favorable CF Environment and Interactions of CF with Electrophiles

Jacob Olsen, David W. Banner, Paul Seiler, +6

ChemBioChem

Quantification of Cation–π Interactions in Protein–Ligand Complexes: Crystal‐Structure Analysis of Factor Xa Bound to a Quaternary Ammonium Ion Ligand

K. Schärer, Martin Morgenthaler, Ralph Paulini, +6

Angewandte Chemie International Edition

EngineeringChemical AnalysisTheoretical Inorganic ChemistryAromatic BoxTrp 215 +18

A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: effects of fluorine substitution on pK_aand binding affinity and evidence for intermolecular C–F⋯CN interactions

Jacob Olsen, Paul Seiler, Björn Wagner, +7

Organic & Biomolecular Chemistry

A Fluorine Scan at the Catalytic Center of Thrombin: CF, COH, and COMe Bioisosterism and Fluorine Effects on p<i>K</i>_a and log <i>D</i> Values

Eliane Schweizer, Anja Hoffmann‐Röder, K. Schärer, +7

ChemMedChem

Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib

U. Obst-Sander, Antônio Ricci, Bernd Kuhn, +22

Journal of Medicinal Chemistry

Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors

Katrin Groebke Zbinden, U. Obst-Sander, Kurt Hilpert, +11

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceMedicinePharmacological AgentPharmacotherapy +2

Multipolar interactions in the D pocket of thrombin: large differences between tricyclic imide and lactam inhibitors

Eliane Schweizer, Anja Hoffmann‐Röder, Jacob Olsen, +6

Organic & Biomolecular Chemistry

Pharmaceutical SciencePeptide SciencePharmacotherapyChemical BiologyPharmaceutical Chemistry +22

Mapping the Fluorophilicity of a Hydrophobic Pocket: Synthesis and Biological Evaluation of Tricyclic Thrombin Inhibitors Directing Fluorinated Alkyl Groups into the P Pocket

Anja Hoffmann‐Röder, Eliane Schweizer, J. Egger, +6

ChemMedChem

Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity

Katrin Groebke Zbinden, David W. Banner, Kurt Hilpert, +6

Bioorganic & Medicinal Chemistry

ThrombosisCardiovascular DiseaseBlood PlateletMedicineHematology +9

Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors

Holger Kühne, U. Obst-Sander, Bernd Kuhn, +11

Bioorganic & Medicinal Chemistry Letters

Dual Fatty AcidMedicinal ChemistryLipid SynthesisBiochemistryNatural Sciences +6