A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types

Stephen M. F. Jamieson, Jack U. Flanagan, Sharada Kolekar, +9

Biochemical Journal

Tumour GrowthCancer BiologyResponsive Cell LinesTumor BiologyMolecular Pharmacology +19

Synthesis and Biological Evaluation of Novel Analogues of the Pan Class I Phosphatidylinositol 3-Kinase (PI3K) Inhibitor 2-(Difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1<i>H</i>-benzimidazole (ZSTK474)

Gordon W. Rewcastle, Swarna A. Gamage, Jack U. Flanagan, +13

Journal of Medicinal Chemistry

Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth

Melanie Sweetlove, Emma Wrightson, Sharada Kolekar, +4

Frontiers in Oncology

Cell ProliferationTumor BiologyMek InhibitorsSignaling PathwayReceptor Tyrosine Kinase +16

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR

Jackie D. Kendall, Anna C. Giddens, Kit Yee Tsang, +17

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryBenzenesulfonohydrazide SarBiochemistryMedicine +8

Diverse mechanisms activate the PI 3-kinase/mTOR pathway in melanomas: implications for the use of PI 3-kinase inhibitors to overcome resistance to inhibitors of BRAF and MEK

Khanh Bao Tran, Sharada Kolekar, Anower Jabed, +7

BMC Cancer

Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors

Jackie D. Kendall, P. D. T. O’Connor, Andrew J. Marshall, +16

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryMedicineRational Drug DesignAnti-cancer Agent +3

Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474)

Gordon W. Rewcastle, Swarna A. Gamage, Jack U. Flanagan, +13

European Journal of Medicinal Chemistry

Medicinal ChemistryPharmaceutical ScienceDrug TargetBiochemistryMedicine +10

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: Synthesis, biological evaluation and molecular modelling

Andrew J. Marshall, Claire L. Lill, Mindy Chao, +8

Bioorganic & Medicinal Chemistry

Medicinal ChemistryBiochemistryMedicineNatural SciencesRational Drug Design +7

Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors

Gordon W. Rewcastle, Sharada Kolekar, Christina M. Buchanan, +12

Oncotarget

Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

Jackie D. Kendall, Andrew J. Marshall, Anna C. Giddens, +16

MedChemComm

Pi3k InhibitorsBioorganic ChemistryCompound 58Organic ChemistryPharmacotherapy +21