Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer

Scott, Fiona, Fala, Angela M., Pennicott, Lewis E., Reuillon, Tristan D., Massirer, Katlin B., Elkins, Jonathan M. and Ward, Simon E. ORCID: https://orcid.org/0000-0002-8745-8377 2020. Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer. Bioorganic and Medicinal Chemistry Letters 30 (8) , 127040. 10.1016/j.bmcl.2020.127040

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Abstract

Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases (<20%) have been investigated for their therapeutic viability, likely due to the lack of available chemical tools across the kinome. In this work we describe initial efforts in the development of a selective chemical tool for protein kinase N2 (PKN2), a relatively unexplored kinase of interest in several types of cancer. The most successful compound, 5, has a measured IC50 of 0.064 μM against PKN2, with ca. 17-fold selectivity over close homologue, PKN1.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Advanced Research Computing @ Cardiff (ARCCA) Medicine MRC Centre for Neuropsychiatric Genetics and Genomics (CNGG)
Publisher:	Elsevier
ISSN:	0960-894X
Date of First Compliant Deposit:	26 June 2020
Date of Acceptance:	14 February 2020
Last Modified:	05 May 2023 22:29
URI:	https://orca.cardiff.ac.uk/id/eprint/132824

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