Antitumor Activity of HKI-272, an Orally Active, Irreversible Inhibitor of the HER-2 Tyrosine Kinase

Sridhar K. Rabindran, Carolyn Discafani, Edward Rosfjord, +13

Cancer Research

Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity

Hwei‐Ru Tsou, Elsebe G. Overbeek-Klumpers, William Hallett, +13

Journal of Medicinal Chemistry

Medicinal ChemistryBiochemistrySafer Cyclization StepMedicineNatural Sciences +11

6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases with Enhanced Antitumor Activity

Hwei‐Ru Tsou, Nellie Mamuya, Bernard D. Johnson, +12

Journal of Medicinal Chemistry

Combinatorial ChemistryPharmacotherapyPharmaceutical ChemistryTumor BiologyMedicinal Chemistry +16

Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)

Allan Wissner, Elsebe Overbeek, Marvin F. Reich, +16

Journal of Medicinal Chemistry

Combinatorial ChemistryPharmaceutical ScienceBioorganic ChemistryPharmacotherapy6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles +17

4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile Inhibitors of Epidermal Growth Factor Receptor Kinase and Their Bioisosteric Relationship to the 4-Anilino-6,7-dialkoxyquinazoline Inhibitors

Allan Wissner, Dan M. Berger, Diane H. Boschelli, +14

Journal of Medicinal Chemistry

Pharmaceutical ScienceOrganic ChemistryPharmacotherapyDermatologyHeterocycle Chemistry +17

Discovery of 4-(Benzylaminomethylene)isoquinoline-1,3-(2<i>H</i>,4<i>H</i>)-diones and 4-[(Pyridylmethyl)aminomethylene]isoquinoline-1,3-(2<i>H</i>,4<i>H</i>)-diones as Potent and Selective Inhibitors of the Cyclin-Dependent Kinase 4

Hwei‐Ru Tsou, Xiaoxiang Liu, Gary H. Birnberg, +14

Journal of Medicinal Chemistry

Organic ChemistrySelective InhibitorsHeterocycle ChemistryChemical BiologyChemical Derivative +16

Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment

Scott C. Mayer, A. Banker, Frank Boschelli, +11

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineIsoquinolinedione InhibitorsLead IdentificationFibroblast Growth Factor +7

Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents: parallel synthesis for lead optimization of amide region

Ariamala Gopalsamy, Hui Yang, John W. Ellingboe, +7

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineNatural SciencesRational Drug DesignOrganic Chemistry +9

4-(Phenylaminomethylene)isoquinoline-1,3(2<i>H</i>,4<i>H</i>)-diones as Potent and Selective Inhibitors of the Cyclin-Dependent Kinase 4 (CDK4)

Hwei‐Ru Tsou, Mercy Otteng, Tritin Tran, +10

Journal of Medicinal Chemistry

Chemoprevention StrategySelective InhibitorsHeterocycle ChemistryPharmaceutical ChemistryMolecular Pharmacology +14

Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents

Allan Wissner, M. Brawner Floyd, Sridhar K. Rabindran, +5

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmacologyTherapeutic Antitumor AgentsPharmacological AgentPharmacotherapy +7