title: Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.
abstract: PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors applying a scaffold hopping approach. Initial exploration around this scaffold and X-ray crystallographic data are hereby described.
authors.affiliation: Experimental Therapeutics Program, Spanish National Cancer Research Centre (CNIO), Madrid, Spain. jpastor@cnio.es
authors.forename: Joaquín
authors.initials: J
authors.lastname: Pastor
authors.forename: Julen
authors.initials: J
authors.lastname: Oyarzabal
authors.forename: Gustavo
authors.initials: G
authors.lastname: Saluste
authors.forename: Rosa María
authors.initials: RM
authors.lastname: Alvarez
authors.forename: Virginia
authors.initials: V
authors.lastname: Rivero
authors.forename: Francisco
authors.initials: F
authors.lastname: Ramos
authors.forename: Elena
authors.initials: E
authors.lastname: Cendón
authors.forename: Carmen
authors.initials: C
authors.lastname: Blanco-Aparicio
authors.forename: Nuria
authors.initials: N
authors.lastname: Ajenjo
authors.forename: Antonio
authors.initials: A
authors.lastname: Cebriá
authors.forename: M I
authors.initials: MI
authors.lastname: Albarrán
authors.forename: David
authors.initials: D
authors.lastname: Cebrián
authors.forename: Ana
authors.initials: A
authors.lastname: Corrionero
authors.forename: Jesús
authors.initials: J
authors.lastname: Fominaya
authors.forename: Guillermo
authors.initials: G
authors.lastname: Montoya
authors.forename: Marco
authors.initials: M
authors.lastname: Mazzorana
mesh_terms: D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D047428:Protein Kinase Inhibitors; D011725:Pyridines; D014230:Triazoles; D051573:Proto-Oncogene Proteins c-pim-1; C406031:proto-oncogene proteins pim