Bioorganic & Medicinal Chemistry Letters ——个性化文献订阅—

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

作者	Bebbington, D; Binch, H; Charrier, JD; Everitt, S; Fraysse, D; Golec, J; Kay, D; Knegtel, R; Mak, C; Mazzei, F; Miller, A; Mortimore, M; O'Donnell, M; Patel, S; Pierard, F; Pinder, J; Pollard, J; Ramaya, S; Robinson, D; Rutherford, A; Studley, J; Westcott, J

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2009年19-13; 页码 3586-3592

关联知识点

[摘要]：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 modi. cation 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. (C) 2009 Elsevier Ltd. All rights reserved.
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