Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers

Julien P. N. Papillon, Katsumasa Nakajima, Christopher D. Adair, +33

Journal of Medicinal Chemistry

Brahma HomologMolecular BiologyCancer BiologyTumor BiologyTranscriptional Regulation +17

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer

Matthew J. LaMarche, Michael Acker, Andreea Argintaru, +61

Journal of Medicinal Chemistry

<i>N</i>-Hydroxy-3-phenyl-2-propenamides as Novel Inhibitors of Human Histone Deacetylase with in Vivo Antitumor Activity:  Discovery of (2<i>E</i>)-<i>N</i>-Hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1<i>H</i>-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824)

Stacy Remiszewski, Lidia Sambucetti, Kenneth W. Bair, +28

Journal of Medicinal Chemistry

PathologyPharmacotherapyPharmaceutical ChemistryTumor BiologyMedicinal Chemistry +15

Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Michael D. Shultz, Atwood K. Cheung, C.A. Kirby, +25

Journal of Medicinal Chemistry

Drug TargetSelective Tankyrase InhibitorsPharmacotherapyChemical BiologyPharmaceutical Chemistry +16

4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6

Young Shin Cho, Maria Borland, Christopher T. Brain, +18

Journal of Medicinal Chemistry

Cyclin-dependent Kinase 4/6Combinatorial ChemistryMedicinal ChemistryBioorganic ChemistryBiochemistry +13

Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors

Jeffrey T. Bagdanoff, Zhouliang Chen, Michael Acker, +23

Journal of Medicinal Chemistry

Medicinal ChemistrySignaling PathwayReceptor Tyrosine KinaseCell SignalingProtein Function +14

Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight

B. Barry Touré, J. Giraldes, Troy Smith, +22

Journal of Medicinal Chemistry

Selective InhibitorsCell CyclePreliminary Biology InsightTumor BiologyEmbryology +15

Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors

Young Shin Cho, Hayley C. Angove, Christopher T. Brain, +33

ACS Medicinal Chemistry Letters

Drug TargetChemical BiologyPharmaceutical ChemistryMedicinal ChemistryReceptor Tyrosine Kinase +16

Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1

Julian Levell, Thomas R. Caferro, Gregg Chenail, +25

ACS Medicinal Chemistry Letters

The Discovery of SWI/SNF Chromatin Remodeling Activity as a Novel and Targetable Dependency in Uveal Melanoma

Florencia Rago, GiNell Elliott, Ailing Li, +24

Molecular Cancer Therapeutics