| Literature DB >> 19447622 |
David Bebbington1, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Julian Golec, David Kay, Ronald Knegtel, Chau Mak, Francesca Mazzei, Andrew Miller, Michael Mortimore, Michael O'Donnell, Sanjay Patel, Francoise Pierard, Joanne Pinder, John Pollard, Sharn Ramaya, Daniel Robinson, Alistair Rutherford, John Studley, James Westcott.
Abstract
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.Entities:
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Year: 2009 PMID： 19447622 DOI： 10.1016/j.bmcl.2009.04.136
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823