Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (<i>R</i>)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2<i>H</i>)-one (PF-06821497)

Pei‐Pei Kung, Patrick Bingham, Alexei Brooun, +38

Journal of Medicinal Chemistry

Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer

Kevin D. Freeman‐Cook, Robert L. Hoffman, Douglas C. Behenna, +30

Journal of Medicinal Chemistry

Dihydroxyphenylisoindoline Amides as Orally Bioavailable Inhibitors of the Heat Shock Protein 90 (Hsp90) Molecular Chaperone

Pei‐Pei Kung, Buwen Huang, Gang Zhang, +15

Journal of Medicinal Chemistry

Pharmaceutical ScienceChemical BiologyPharmaceutical ChemistryMedicinal ChemistryChaperones +14

Chemogenetic Evaluation of the Mitotic Kinesin CENP-E Reveals a Critical Role in Triple-Negative Breast Cancer

Pei‐Pei Kung, Ricardo Martínez, Zhou Zhu, +18

Molecular Cancer Therapeutics

Breast OncologyCancer BiologyTumor BiologySpindle Assembly CheckpointBreast Cancer Patients +16

Discovery of Novel Disaccharide Antibacterial Agents Using a Combinatorial Library Approach

Michael J. Sofia, Nigel M. Allanson, Nicole T. Hatzenbuhler, +23

Journal of Medicinal Chemistry

Antibiotic AdjuvantAltmetric Attention ScoreAntimicrobial ChemotherapyDrug ResistanceAntimicrobial Stewardship +15

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2 <i>H</i> )-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

Pei‐Pei Kung, Eugene Rui, Simon Bergqvist, +34

Journal of Medicinal Chemistry

Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone

Pei‐Pei Kung, P.-J. Sinnema, Paul Richardson, +10

Bioorganic & Medicinal Chemistry Letters

EngineeringProtein AssemblyBiophysicsProtein FoldingMedicine +12

Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-Containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-Amino-4-{4-chloro-2-[2-(4-fluoro-1<i>H</i>-pyrazol-1-yl)ethoxy]-6-methylphenyl}-<i>N</i>-(2,2-difluoropropyl)-5,7-dihydro-6<i>H</i>-pyrrolo[3,4-<i>d</i>]pyrimidine-6-carboxamide

Luke R. Zehnder, Michael J. Bennett, Jerry Meng, +23

Journal of Medicinal Chemistry

Pharmaceutical ScienceDevelopment CandidatePharmacotherapyPharmaceutical ChemistryTumor Biology +16

Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195)

Hengmiao Cheng, Suvi T. M. Orr, Simon Bailey, +36

Journal of Medicinal Chemistry

Synthesis of Aryl Ethers via a Sulfonyl Transfer Reaction

Neal W. Sach, Daniel T. Richter, Stephan J. Cripps, +5

Organic Letters

Cross-coupling ReactionAryl EthersEngineeringAlkene MetathesisOrganic Chemistry +6