Anticancer RuII and RhIII Piano-Stool Complexes that are Histone Deacetylase Inhibitors

Jasmine M Cross; Tim R Blower; Natalie Gallagher; Jason H Gill; Kimberly L Rockley; James W Walton

doi:10.1002/cplu.201600413

Anticancer Ru^II and Rh^III Piano-Stool Complexes that are Histone Deacetylase Inhibitors

Chempluschem. 2016 Dec;81(12):1276-1280. doi: 10.1002/cplu.201600413. Epub 2016 Oct 12.

Authors

Jasmine M Cross¹, Tim R Blower², Natalie Gallagher³, Jason H Gill³, Kimberly L Rockley³, James W Walton¹

Affiliations

¹ Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, United Kingdom.
² School of Biological and Biomedical Sciences, Durham University, South Road, Durham, DH1 3LE, United Kingdom.
³ School of Medicine, Pharmacy and Health, Durham University, Wolfson Research Institute, Queen's Campus, Stockton on Tees, TS17 6BH, United Kingdom.

PMID: 31964062
DOI: 10.1002/cplu.201600413

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.

Keywords: antitumour agents; bioorganometallic chemistry; histone deacetylase inhibitors; piano-stool complexes; ruthenium.