Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

Tara Rheault, John Stellwagen, George M. Adjabeng, +15

ACS Medicinal Chemistry Letters

B-raf-driven TumorsAntitumor ActivityHyperactive SignalingTumor BiologyMedicinal Chemistry +14

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

Kimberly G. Petrov, Yuemei Zhang, Malcolm Carter, +9

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryDrug TargetBiochemistryNatural SciencesMedicine +9

Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles

Edgar R. Wood, Lee F. Kuyper, Kimberly G. Petrov, +3

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceBiochemistryMedicineNatural Sciences +8

6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases

Edgar R. Wood, Lisa M. Shewchuk, Byron Ellis, +22

Proceedings of the National Academy of Sciences

Combinatorial ChemistryMedicinal ChemistryBiochemistryCovalent BondMedicine +11

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors

Tara Rheault, Thomas R. Caferro, Scott H. Dickerson, +13

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePharmacotherapyAnti-cancer AgentDrug Development +3

Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors

Alex G. Waterson, Kimberly G. Petrov, Keith R. Hornberger, +13

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryAniline HeadgroupsBiochemistryMedicine +7

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

John Stellwagen, George M. Adjabeng, Marc R. Arnone, +12

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPotent B-rafv600e InhibitorsMedicineRational Drug DesignDrug Development +3

Substrate Specificity and Novel Selective Inhibitors of TNF-α Converting Enzyme (TACE) from Two-Dimensional Substrate Mapping

Millard H. Lambert, Robert J. Blackburn, Theresa Seaton, +17

Combinatorial Chemistry & High Throughput Screening

Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors

Kirk L. Stevens, Krystal J. Alligood, Jennifer G. Badiang Alberti, +19

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryStereochemical EffectsMedicineNatural Sciences +8

Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2

Curt D. Haffner, Stephen A. Thomson, Yu Guo, +11

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryMedicineIon ChannelsPharmacology