Perfluorinated HDAC inhibitors as Selective Anticancer Agents

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

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
• Public URL: https://durham-repository.worktribe.com/output/1342378