Anticancer RuII and RhIII Piano‐Stool Complexes that are Histone Deacetylase Inhibitors. Issue 12 (12th October 2016)

• Record Type: Journal Article
• Authors: Cross, Jasmine M.; Blower, Tim R.; Gallagher, Natalie; Gill, Jason H.; Rockley, Kimberly L.; Walton, James W.
• Is Part Of: ChemPlusChem. Volume 81:Issue 12(2016)
• Page Start: 1276
• Page End: 1280
• Publication Date: 2016-10-12
• Subjects: antitumour agents -- bioorganometallic chemistry -- histone deacetylase inhibitors -- piano-stool complexes -- ruthenium; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/cplu.201600413
• Languages: English
• ISSNs: 2192-6506

Abstract

Abstract: The first examples of Ru II and Rh III piano‐stool complex histone deacetylase (HDAC) inhibitors are presented. The novel complexes have antiproliferative activity against H460 non‐small‐cell lung carcinoma cells that is comparable to the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (SAHA). Strong evidence for HDAC inhibition as a primary mechanism of action is provided. The complexes reported here represent an important step towards the design of highly active and selective HDAC inhibitors. Abstract : Tickle the ivories : The first examples of piano‐stool complexes of Ru II and Rh III to show histone deacetylase (HDAC) inhibition are presented. The novel complexes exhibited anticancer activity comparable to the HDAC inhibitor SAHA used in the clinic. Strong evidence for HDAC inhibition as a primary mechanism of action is provided (see graph) and covalent binding to DNA is ruled out.