Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

Janeta Popovici-Müller, René M. Lemieux, Erin Artin, +33

ACS Medicinal Chemistry Letters

Idh1 Mutant CancersSomatic Point MutationsSomatic VariantOncogenic AgentMedicine +12

Discovery of <i>N</i>-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily

Gretchen M. Schroeder, Yongmi An, Zhen‐Wei Cai, +28

Journal of Medicinal Chemistry

Orally Efficacious InhibitorDrug TargetPharmacotherapyPharmaceutical ChemistryTumor Biology +19

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

Zenon Konteatis, Erin Artin, Brandon Nicolay, +25

ACS Medicinal Chemistry Letters

Mutant Isocitrate DehydrogenaseHigh-grade GliomasGliomaNeuro-oncologyMedicinal Chemistry +16

Discovery of Brivanib Alaninate ((<i>S</i>)-((<i>R</i>)-1-(4-(4-Fluoro-2-methyl-1<i>H</i>-indol-5-yloxy)-5-methylpyrrolo[2,1-<i>f</i>][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215)

Zhen‐Wei Cai, Yongzheng Zhang, R. M. Borzilleri, +21

Journal of Medicinal Chemistry

Pharmaceutical ScienceOral BioavailabilityL-alanine Prodrug 8PharmacotherapyPharmaceutical Chemistry +18

Discovery and Preclinical Studies of (<i>R</i>)-1-(4-(4-Fluoro-2-methyl-1<i>H</i>-indol-5-yloxy)-5- methylpyrrolo[2,1-<i>f</i>][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an In Vivo Active Potent VEGFR-2 Inhibitor

Rajeev S. Bhide, Zhen‐Wei Cai, Yong‐Zheng Zhang, +25

Journal of Medicinal Chemistry

Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities

Kyoung Soon Kim, Liping Zhang, Robert J. Schmidt, +23

Journal of Medicinal Chemistry

Drug TargetBiological ActivitiesChemical BiologyPharmaceutical ChemistryCompound 2 +17

The Antiangiogenic Activity in Xenograft Models of Brivanib, a Dual Inhibitor of Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinases

Rajeev S. Bhide, Louis J. Lombardo, John T. Hunt, +12

Molecular Cancer Therapeutics

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors

Zhen‐Wei Cai, Donna Wei, Gretchen M. Schroeder, +16

Bioorganic & Medicinal Chemistry Letters

Pharmaceutical ScienceBiochemistryMedicineNatural SciencesRational Drug Design +6

Design, Synthesis, and Evaluation of Orally Active 4-(2,4-Difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-<i>f</i>][1,2,4]triazines as Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Inhibitors

R. M. Borzilleri, Xiaoping Zheng, Ligang Qian, +15

Journal of Medicinal Chemistry

Enzyme KineticsMedicinal ChemistryPharmaceutical ScienceBiochemistryMedicine +12

A Study of the Favorskii Rearrangement with 3-Bromo-4-oxo-2,2,6,6-tetramethylpiperidine-1-oxyl

George Sosnovsky, Zhen‐Wei Cai

The Journal of Organic Chemistry

Chemical MeasurementChemical AnalysisAltmetric Attention ScoreChemometricsOrganic Chemistry +8