2011
Aryl extensions of thienopyrimidinones as fibroblast growth factor receptor 1 kinase inhibitors
Ekkati AR, Mandiyan V, Ravindranathan KP, Bae J, Schlessinger J, Jorgensen WL. Aryl extensions of thienopyrimidinones as fibroblast growth factor receptor 1 kinase inhibitors. Tetrahedron Letters 2011, 52: 2228-2231. PMID: 21516197, PMCID: PMC3079261, DOI: 10.1016/j.tetlet.2010.12.081.Peer-Reviewed Original ResearchInhibition of phosphorylationKinase inhibitorsFGFR1Propionic acid groupsThienopyrimidinone derivativesInhibitorsPhosphorylation
2010
Discovery of Novel Fibroblast Growth Factor Receptor 1 Kinase Inhibitors by Structure-Based Virtual Screening
Ravindranathan KP, Mandiyan V, Ekkati AR, Bae JH, Schlessinger J, Jorgensen WL. Discovery of Novel Fibroblast Growth Factor Receptor 1 Kinase Inhibitors by Structure-Based Virtual Screening. Journal Of Medicinal Chemistry 2010, 53: 1662-1672. PMID: 20121196, PMCID: PMC2842983, DOI: 10.1021/jm901386e.Peer-Reviewed Original ResearchConceptsFibroblast growth factorCo-crystal structureKinase structureFGFR1 kinaseSearch of inhibitorsEmbryonic developmentProtein structureAlternative conformationsCell proliferationStructural motifsKinase inhibitorsGrowth factorNew structural motifDiverse compoundsVirtual screeningFGFR1InhibitorsDockingWound healingThienopyrimidinone derivativesImportant roleConformationKinaseProteinMotif