Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells

Bruce Grasberger, Tianbao Lu, Carsten J. Schubert, +23

Journal of Medicinal Chemistry

Molecular BiologyChemical BiologyPharmaceutical ChemistryTumor BiologyMolecular Pharmacology +18

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR

Daniel J. Parks, Louis V. LaFrance, Raul R. Calvo, +10

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyDrug TargetSmall Molecule AntagonistsMedicineNatural Sciences +9

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation <i>in vitro</i> and sensitize tumors to doxorubicin <i>in vivo</i>

Holly K. Koblish, Shuyuan Zhao, Carol F. Franks, +16

Molecular Cancer Therapeutics

P53 InteractionChemoprevention StrategyP53 ComplexTumor BiologyMedicinal Chemistry +16

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design

Daniel J. Parks, Louis V. LaFrance, Raul R. Calvo, +14

Bioorganic & Medicinal Chemistry Letters

Hdm2-p53 Protein–protein InteractionDrug TargetMedicineRational Drug DesignStructure-based Drug Design +5

Design, Synthesis, and Biological Evaluation of Novel Potent and Selective α_vβ₃/α_vβ₅ Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core

Juan Marugán, Carl L. Manthey, Beth Anaclerio, +8

Journal of Medicinal Chemistry

Improved BioavailabilityPharmaceutical ScienceSelective AlphaNovel PotentPharmacotherapy +15

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity

Kristi Leonard, Juan Marugán, Pierre Raboisson, +9

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyFunctional SelectivityMedicineMechanism Of ActionPharmacological Agent +4

7-Fluoroindazoles as Potent and Selective Inhibitors of Factor Xa

Yu‐Kai Lee, Daniel J. Parks, Tianbao Lu, +12

Journal of Medicinal Chemistry

Bioorganic ChemistryPharmacotherapyChemical BiologyPharmaceutical ChemistryMedicinal Chemistry +14

Glucose-6-Phosphate Isomerase (G6PI) Mediates Hypoxia-Induced Angiogenesis in Rheumatoid Arthritis

Ying Lü, Shanshan Yu, Ming Zong, +5

Scientific Reports

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists

Pierre Raboisson, Juan Marugán, Carsten J. Schubert, +10

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryMedicineNatural Sciences +8

Glucose-6-phosphate isomerase promotes the proliferation and inhibits the apoptosis in fibroblast-like synoviocytes in rheumatoid arthritis

Ming Zong, Tianbao Lu, Shasha Fan, +5

Arthritis Research & Therapy

InflammationRheumatologyRheumatoid DisorderAnti-inflammatoryAutoimmune Disease +13