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Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors

Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors

Spencer, John, Amin, Jahangir, Boddiboyena, Ramesh, Packham, Graham, Cavell, Breeze E., Alwi, Sharifah S. Syed, Paranal, Ronald M., Heightman, Tom D., Wang, Minghua, Marsden, Brian, Coxhead, Peter, Guille, Matthew, Tizzard, Graham J., Coles, Simon J. and Bradner, James E, (2012) Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors. Medicinal Chemistry Communication, 3 (1). pp. 61-64. ISSN 2040-2503 (online) (doi:10.1039/c1md00203a)

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Abstract

A small library of ferrocene-based 1,2,3-triazole-containing hydroxamic acids has been synthesised employing click chemistry: 7-(4-ferrocenyl-1H-1,2,3-triazol-1-yl)-N-hydroxyheptanamide, 4b, containing the 1,2,3-triazole moiety adjacent to the ferrocene group, displayed excellent HDAC inhibition and activity in cells, inhibiting the deacetylation of tubulin as well as inducing cell cycle arrest.

Item Type: Article
Uncontrolled Keywords: ferrocene-based 1,2,3-triazole-containing hydroxamic acids, click chemistry, HDAC inhibition and activity
Subjects: R Medicine > R Medicine (General)
R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Faculty / Department / Research Group: Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Related URLs:
Last Modified: 06 Dec 2016 16:05
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/7592

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