Fragment-Hopping-Based Discovery of a Novel Chemical Series of Proto-Oncogene PIM-1 Kinase Inhibitors

PLoS ONE

Volumn 7, Issue 10, 2012, Pages

  Saluste, Gustavo ^a   Albarran, Maria I ^a   Alvarez, Rosa M ^a   Rabal, Obdulia ^a,b   Ortega, Miguel Angel ^a   Blanco, Carmen ^a   Kurz, Guido ^a,c   Salgado, Antonio ^a   Pevarello, Paolo ^a,d   Bischoff, James R ^a,e   Pastor, Joaquin ^a   Oyarzabal, Julen ^a,b  

^a Structural Biology and Biocomputing Programme   (Spain)

^b UNIVERSITY OF NAVARRA   (Spain)

^c ORYZON GENOMICS   (Spain)

^d San Raffaele Biomedical Science Park   (Italy)

^e JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

(1 METHYL PIPERIDIN 4 YLMETHYL) [3 (3 TRIFLUOROMETHOXY PHENYL) 3H (1,2,3,)TRIAZOLO(4,5 B)PYRIDIN 5 YL]AMINE; (6 CHLORO 3 NITRO PYRIDIN 2 YL) (3 TRIFLUOROMETHOXY PHENYL)AMINE; 3 (4 METHOXY PHENYL) 3,4 DIHYDRO (1,2,3)TRIAZOLO(4,5 B)PYRIDIN 5 ONE; 4 [5 (4 FLUORO BENZYLAMINO) (1,2,3)TRIAZOLO(4,5 B)PYRIDIN 3 YL]PHENOL; 4 FLUORO BENZYL [3 (4 METHOXY PHENYL) 3H (1,2,3)TRIAZOLO (4,5 B)PYRIDIN 5 YL]AMINE; 5 CHLORO 3 (3 TRIFLUOROMETHOXY PHENYL) 3H (1,2,3,)TRIAZOLO(4,5 B)PYRIDINE; 6 CHLORO N 2 (3 TRIFLUOROMETHOXY PHENYL)PYRIDINE 2,3 DIAMINE; ETP 39010; K 00135; PROTEIN SERINE THREONINE KINASE INHIBITOR; PROVIRUS INTEGRATION SITE FOR MOLONY LEUKEMIA VIRUS 1 KINASE INHIBITOR; SGI 1776; UNCLASSIFIED DRUG;

ARTICLE; CHEMOGENOMICS; COMPUTER MODEL; DRUG ABSORPTION; DRUG ACTIVITY; DRUG DEVELOPMENT; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG SCREENING; DRUG SELECTIVITY; DRUG STABILITY; DRUG STRUCTURE; FRAGMENT HOPPING BASED DRUG DISCOVERY; IC 50; LIVER MICROSOME; PHARMACOGENOMICS; PHASE 1 CLINICAL TRIAL (TOPIC); PROSPECTIVE STUDY;

DATABASES, PHARMACEUTICAL; DRUG DISCOVERY; HUMANS; INHIBITORY CONCENTRATION 50; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-PIM-1;

EID: 84868110960     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0045964     Document Type: Article

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