Design, synthesis and characterization of “clickable” 4-anilinoquinazoline kinase inhibitors

B. Gayani K. Perera; Dustin J. Maly

doi:10.1039/B720014E

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Molecular BioSystems

Issue 6, 2008

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Design, synthesis and characterization of “clickable” 4-anilinoquinazoline kinase inhibitors

B. Gayani K. Perera and Dustin J. Maly

Mol. BioSyst., 2008, 4, 542-550

DOI: 10.1039/B720014E
Received 08 Jan 2008, Accepted 11 Mar 2008
First published on the web 16 Apr 2008

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Immobilized kinase inhibitors have emerged as powerful reagents for the determination of kinase inhibitor selectivity and for the enrichment of protein targets from cellular lysates. Here, we report the design and synthesis of a set of “clickable” 4-anilinoquinazoline kinase inhibitors. We demonstrate that the attachment of a flexible tether that contains a bio-orthogonal azide functionality does not adversely affect the potency or selectivity of these inhibitors. Furthermore, we demonstrate the utility of these inhibitors through the generation of an affinity matrix for the enrichment of interacting proteins from cellular lysates.

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Molecular BioSystems

Design, synthesis and characterization of “clickable” 4-anilinoquinazoline kinase inhibitors

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