Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases

Matthews, Thomas P., McHardy, Tatiana, Klair, Suki, Boxall, Kathy, Fisher, Martin, Cherry, Michael, Allen, Charlotte E., Addison, Glynn J., Ellard, John, Aherne, G. Wynne, and others. (2010) Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases. Bioorganic & Medicinal Chemistry Letters, 20 (14). pp. 4045-4049. ISSN 0960-894X. (doi:10.1016/j.bmcl.2010.05.096) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:58572)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL: http://doi.org/10.1016/j.bmcl.2010.05.096

Abstract

A range of 3,6-di(hetero)arylimidazo[1,2-a]pyrazine ATP-competitive inhibitors of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogues with improved potency and ligand efficiency against CHK1. Kinase profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to represent a general kinase inhibitor scaffold.

Item Type:	Article
DOI/Identification number:	10.1016/j.bmcl.2010.05.096
Uncontrolled keywords:	CHK1; Kinase inhibitors; Imidazopyrazines
Subjects:	Q Science
Divisions:	Divisions > Division of Natural Sciences > Biosciences
Depositing User:	Michelle Garrett
Date Deposited:	11 Nov 2016 11:14 UTC
Last Modified:	05 Nov 2024 10:49 UTC
Resource URI:	https://kar.kent.ac.uk/id/eprint/58572 (The current URI for this page, for reference purposes)

University of Kent Author Information

Garrett, Michelle D..

Creator's ORCID:	https://orcid.org/0000-0002-3939-1673
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