Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 4, 2012, Pages 1591-1597

  Pastor, Joaquín ^a   Oyarzabal, Julen ^a,b   Saluste, Gustavo ^a   Alvarez, Rosa María ^a   Rivero, Virginia ^a   Ramos, Francisco ^a   Cendón, Elena ^a   Blanco Aparicio, Carmen ^a   Ajenjo, Nuria ^a   Cebriá, Antonio ^a   Albarran M I ^a   Cebrián, David ^a   Corrionero, Ana ^a   Fominaya, Jesús ^a   Montoya, Guillermo ^a   Mazzorana, Marco ^a,c  

^a Centro Nacional de Investigaciones Oncológicas   (Spain)

^b UNIVERSITY OF NAVARRA   (Spain)

^c DIAMOND LIGHT SOURCE LTD   (United Kingdom)

Author keywords

Crystal structure Docking; FLT 3; HERG Binding; Hit to lead; Mechanism of action; Phosphorylation of BAD; PIM inhibitors; Scaffold hopping; Triazolopyridine

Indexed keywords

1,2,3 TRIAZOLO[4,5 B]PYRIDINE; CYTOCHROME P450; IMIDAZOPYRIDINE DERIVATIVE; PROTEIN KINASE PIM 1; PROTEIN SERINE THREONINE KINASE INHIBITOR; TRIAZOLOPYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG;

AMINATION; ARTICLE; CELL PERMEABILIZATION; CELL PROLIFERATION; CELL SURVIVAL; CHEMICAL STRUCTURE; CONTROLLED STUDY; CYTOKINE PRODUCTION; DRUG BINDING SITE; DRUG DEVELOPMENT; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; HYDROGEN BOND; HYDROPHOBICITY; IC 50; PHARMACOKINETICS; PHYSICAL CHEMISTRY; PLASMA CLEARANCE; PLASMA HALF LIFE; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

EID: 84856663843     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.12.130     Document Type: Article

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