Article ID Journal Published Year Pages File Type
1366552 Bioorganic & Medicinal Chemistry Letters 2007 6 Pages PDF
Abstract

The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. Based on the 4-anilinoquinazoline chemotype, the syntheses of several new series of erbB2 inhibitors are described with quinazoline and pyrido[4,3-d]pyrimidine cores. The vast majority of these compounds are found to be >100× selective over the closely related EGFR kinase. Two lead compounds are further shown to have low clearance and moderate bioavailability in rat.

Graphical abstractThe synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. The vast majority of these compounds are found to be >100× selective over the closely related EGFR kinase. Two lead compounds are further shown to have low clearance and moderate bioavailability in rat.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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