Perfluorinated HDAC inhibitors as selective anticancer agents. Issue 43 (26th October 2017)

• Record Type: Journal Article
• Authors: Walton, James W.; Cross, Jasmine M.; Riedel, Tina; Dyson, Paul J.
• Is Part Of: Organic & biomolecular chemistry. Volume 15:Issue 43(2017)
• Page Start: 9186
• Page End: 9190
• Publication Date: 2017-10-26
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c7ob02339a
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : Perfluorinated histone deacetylase inhibitors show more potent cytotoxicity and greater selectivity towards ovarian carcinoma cells over human embryonic kidney cells, compared to the clinically-approved inhibitor, SAHA. Abstract : A series of potent histone deacetylase inhibitors is presented that incorporate alkyl or perfluorinated alkyl chains. Several new compounds show greater in vitro antiproliferative 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.