Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells

Bagley, Mark Christopher, Davis, Terence ORCID: https://orcid.org/0000-0003-2780-0262, Dix, Matthew, Rokicki, Michal Jaroslaw and Kipling, David Glyn 2007. Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Biorganic and Medicinal Chemistry Letters 17 (18) , pp. 5107-5110. 10.1016/j.bmcl.2007.07.016

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Abstract

The p38 mitogen-activated protein kinase inhibitor VX-745 is prepared rapidly and efficiently in a four-step sequence using a combination of conductive heating and microwave-mediated steps. Its inhibitory activity was confirmed in hTERT immortalized HCA2 and WS dermal fibroblasts at 0.5–1.0 μM concentration by ELISA and immunoblot assay, and displays excellent kinase selectivity over the related stress-activated kinase JNK.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Chemistry Medicine
Subjects:	Q Science > QD Chemistry R Medicine > RB Pathology
Uncontrolled Keywords:	p38 MAPK; Werner syndrome; VX-745; Microwaves; Heterocycles; Ullmann coupling; Palladium
Publisher:	Elsevier
ISSN:	0960-894X
Last Modified:	14 Dec 2022 02:15
URI:	https://orca.cardiff.ac.uk/id/eprint/46652

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