کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365720 | 981570 | 2007 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Observations from two structurally related series of KSP inhibitors led to the proposal and discovery of dihydropyrazolobenzoxazines that possess ideal properties for cancer drug development. The synthesis and characterization of this class of inhibitors along with relevant pharmacokinetic and in vivo data are presented. The synthesis is highlighted by a key [3+2] cycloaddition to form the pyrazolobenzoxazine core followed by diastereospecific installation of a quaternary center.
Dihydropyrazolobenzoxazines (i.e., 20) are reported as potent inhibitors of the mitotic kinesin KSP.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5671–5676
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5671–5676
نویسندگان
Robert M. Garbaccio, Edward S. Tasber, Lou Anne Neilson, Paul J. Coleman, Mark E. Fraley, Christy Olson, Jeff Bergman, Maricel Torrent, Carolyn A. Buser, Keith Rickert, Eileen S. Walsh, Kelly Hamilton, Robert B. Lobell, Weikang Tao, Vicki J. South,