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Microwave-assisted synthesis of a pyrazolyl ketone library for evaluation as p38 MAPK inhibitors in Werner syndrome cells

Bagley, Mark Christopher, Davis, Terence, Dix, Matthew Charles, Murziani, Paola G. S., Rokicki, Michal Jaroslaw and Kipling, David Glyn 2010. Microwave-assisted synthesis of a pyrazolyl ketone library for evaluation as p38 MAPK inhibitors in Werner syndrome cells. Future Medicinal Chemistry 2 (2) , pp. 203-213. 10.4155/fmc.09.160

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Abstract

Background: The pyrazolyl ketone motif of RO3201195, which exhibits good oral bioavailability and high selectivity for p38 MAPK over other kinases, is a key pharmacophore that could find application in the treatment of Werner syndrome. Results and discussion: Microwave irradiation promotes Knoevenagel condensation of a β-ketonitrile and formamidine, to give β-aminovinyl ketones, and their subsequent cyclocondensation with a subset of hydrazines to provide rapid access to a 24-membered library of pyrazolyl ketones. The library was evaluated in human hTERT-immortalized HCA2 dermal cells and Werner syndrome cells. Conclusion: Four compounds display comparable, if not slightly improved, potency over RO3201195.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Medicine
Subjects: Q Science > QD Chemistry
R Medicine > R Medicine (General)
Publisher: Future Science Ltd
ISSN: 1756-8919
Last Modified: 10 Oct 2017 13:57
URI: http://orca.cf.ac.uk/id/eprint/21999

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