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

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


The first examples of RuII and RhIII 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.