The discovery of the potent aurora inhibitor MK-0457 (VX-680)

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 13, 2009, Pages 3586-3592

  Bebbington, David ^a   Binch, Hayley ^a   Charrier, Jean Damien ^a   Everitt, Simon ^a   Fraysse, Damien ^a   Golec, Julian ^a   Kay, David ^a   Knegtel, Ronald ^a   Mak, Chau ^a   Mazzei, Francesca ^a   Miller, Andrew ^a   Mortimore, Michael ^a   O'Donnell, Michael ^a   Patel, Sanjay ^a   Pierard, Francoise ^a   Pinder, Joanne ^a   Pollard, John ^a   Ramaya, Sharn ^a   Robinson, Daniel ^a   Rutherford, Alistair ^a   Studley, John ^a   Westcott, James ^a   more..

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

Aurora; Kinase inhibitor; SAR

Indexed keywords

AURORA A KINASE; AURORA B KINASE; AURORA KINASE INHIBITOR; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; GLYCOGEN SYNTHASE KINASE 3BETA; PROTEIN TYROSINE KINASE;

ACUTE LYMPHOBLASTIC LEUKEMIA; ACUTE LYMPHOCYTIC LEUKEMIA; ANTINEOPLASTIC ACTIVITY; ARTICLE; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; CRYSTAL STRUCTURE; DRUG SCREENING; HUMAN; IC 50; MAXIMUM TOLERATED DOSE; NONHUMAN; PHILADELPHIA CHROMOSOME POSITIVE CELL; STRUCTURE ACTIVITY RELATION;

CELL LINE, TUMOR; COMPUTER SIMULATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; MUTANT PROTEINS; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 66349114286     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.04.136     Document Type: Article

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