438203-33-9Relevant academic research and scientific papers
The discovery of the potent aurora inhibitor MK-0457 (VX-680)
Bebbington, David,Binch, Hayley,Charrier, Jean-Damien,Everitt, Simon,Fraysse, Damien,Golec, Julian,Kay, David,Knegtel, Ronald,Mak, Chau,Mazzei, Francesca,Miller, Andrew,Mortimore, Michael,O'Donnell, Michael,Patel, Sanjay,Pierard, Francoise,Pinder, Joanne,Pollard, John,Ramaya, Sharn,Robinson, Daniel,Rutherford, Alistair,Studley, John,Westcott, James
, p. 3586 - 3592 (2009)
The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR is described. Replacement of the initial quinazoline core with a pyrimidine scaffold and modification of substituents led to a series of very potent inhibitors of cellular proliferation. MK-0457 (VX-680) has been assessed in Phase II clinical trials in patients with treatment-refractory chronic myelogenous leukemia (CML) or Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL) containing the T315I mutation.
Pyrazole compounds useful as protein kinase inhibitors
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Page/Page column 129, (2008/06/13)
This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx/sup
