Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365720 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
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.
Graphical abstractDihydropyrazolobenzoxazines (i.e., 20) are reported as potent inhibitors of the mitotic kinesin KSP.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,