کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372244 | 981867 | 2009 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery of the potent aurora inhibitor MK-0457 (VX-680)
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR, which led to the discovery of MK-0457 (VX-680), is described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 13, 1 July 2009, Pages 3586–3592
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 13, 1 July 2009, Pages 3586–3592
نویسندگان
David Bebbington, 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,