Perfluorinated HDAC inhibitors as Selective Anticancer Agents

Walton, James W.; Cross, Jasmine M.; Riedel, Tina; Dyson, Paul

doi:10.1039/c7ob02339a

Perfluorinated HDAC inhibitors as Selective Anticancer Agents

Walton, James W.; Cross, Jasmine M.; Riedel, Tina; Dyson, Paul

Authors

Dr James Walton james.walton@durham.ac.uk
Associate Professor

Jasmine M. Cross

Tina Riedel

Paul Dyson

Abstract

A series of potent histone deacetylase inhibitors is presented that incorporate alkyl or perfluorinated alkyl chains. Several new compounds show greater in vitro antiproliferate activity than the clinically approved inhibitor, SAHA. Furthermore, the new compounds show up to 5-fold greater activity against cancer cells than healthy cells. This selectivity is in contrast to SAHA, which is more active against the healthy cell line than the cancer cell line tested. Finally, we report an increase in activity for SAHA under mild hyperthermia, indicating that it could be an interesting candidate to use in combination with thermal therapy.

Citation

Walton, J. W., Cross, J. M., Riedel, T., & Dyson, P. (2017). Perfluorinated HDAC inhibitors as Selective Anticancer Agents. Organic and Biomolecular Chemistry, 15(43), 9186-9190. https://doi.org/10.1039/c7ob02339a

Journal Article Type	Article
Acceptance Date	Oct 18, 2017
Online Publication Date	Oct 18, 2017
Publication Date	Nov 21, 2017
Deposit Date	Oct 19, 2017
Publicly Available Date	Oct 18, 2018
Journal	Organic and Biomolecular Chemistry
Print ISSN	1477-0520
Electronic ISSN	1477-0539
Publisher	Royal Society of Chemistry
Peer Reviewed	Peer Reviewed
Volume	15
Issue	43
Pages	9186-9190
DOI	https://doi.org/10.1039/c7ob02339a