Article ID Journal Published Year Pages File Type
1365720 Bioorganic & Medicinal Chemistry Letters 2007 6 Pages PDF
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

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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