AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with <i>In vitro</i> and <i>In vivo</i> Antitumor Activity

Christine M. Chresta, Barry R. Davies, Ian Hickson, +21

Cancer Research

Mtorc2 Substrate AktCell DeathPharmacotherapyTumor BiologyMtorc1 Substrates +19

4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2<i>H</i>-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1

Keith Menear, Claire Adcock, Robert Boulter, +17

Journal of Medicinal Chemistry

Medicinal ChemistryPolymerase ActivationOral BioavailabilityPharmaceutical ScienceBiochemistry +13

Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion

Sarah E. Golding, Elizabeth Rosenberg, Nicholas C.K. Valerie, +11

Molecular Cancer Therapeutics

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014

Kurt G. Pike, Karine Malagu, Marc Hummersone, +7

Bioorganic & Medicinal Chemistry Letters

Molecular DockingMedicinal ChemistryDrug TargetBiochemistryMedicine +10

Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K

Joanne M. Munck, Michael A. Batey, Yan Zhao, +15

Molecular Cancer Therapeutics

Dual InhibitorTumor BiologyDna Double-strand BreaksMedicineApoptosis +13

Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase

Vincent M. Loh, Xiaoling Cockcroft, Krystyna J. Dillon, +14

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryNovel SeriesBiochemistryNatural SciencesMedicine +8

Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase

Xiaoling Cockcroft, Krystyna J. Dillon, Lesley Dixon, +6

Bioorganic & Medicinal Chemistry Letters

BiochemistryNatural SciencesBiocatalysisMedicineNovel Potent Inhibitors +8

Pyranone, Thiopyranone, and Pyridone Inhibitors of Phosphatidylinositol 3-Kinase Related Kinases. Structure−Activity Relationships for DNA-Dependent Protein Kinase Inhibition, and Identification of the First Potent and Selective Inhibitor of the Ataxia Telangiectasia Mutated Kinase

Jonathan J. Hollick, Laurent Rigoreau, Céline Cano, +16

Journal of Medicinal Chemistry

Bioorganic ChemistryMolecular BiologyDna-dependent Protein KinaseChemical BiologyMolecular Pharmacology +17

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

Karine Malagu, Heather M. E. Duggan, Keith Menear, +18

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryDrug TargetBiochemistryNatural Sciences +9

Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR

Keith Menear, Sylvie Gomez, Karine Malagu, +15

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryDrug TargetBiochemistryMedicineNatural Sciences +8