Anticancer Ruthenium Complexes with HDAC Isoform Selectivity

Abstract

The histone deacetylase (HDAC) enzymes have emerged as an important class of molecular targets in cancer therapy, with five inhibitors in clinical use. Recently, it has been shown that a lack of selectivity between the 11 Zn-dependent HDAC isoforms may lead to unwanted side-effects. In this paper, we show that piano stool Ru complexes can act as HDAC inhibitors, and variation in the capping arene leads to differences in HDAC isoform selectivity.

Water-soluble copper pyrithione complexes with cytotoxic and antibacterial activity

“…In vitro human cell line cytotoxicity data Metal complexes have been long been explored for their potential anticancer activity. [25][26][27] For the novel copper complexes, antiproliferation studies were carried out against MIA PaCa-2 pancreatic carcinoma cells, 143B bone osteosarcoma cells and normal ARPE-19 retinal epithelial cells, using MTT assay over the course of 24 h. [Cu(PyS) 2 ] and the three novel copper(II) complexes were screened alongside the known anticancer drug cisplatin and CuCl 2 as a reference. The inhibitory concentration (IC 50 ) values of the three PEG-substituted complexes are in the sub-micromolar range and are comparable with that of the parent [Cu(PyS) 2 ] complex (Table 2).…”

Effect of cysteine thiols on the catalytic and anticancer activity of Ru(ii) sulfonyl-ethylenediamine complexes

“…Studies of the antiproliferative activity of organometallic complexes, especially the Ir, 1–3 Os, 4 Rh 5,6 and Ru 7,8 complexes, have been stimulated by the clinical success of platinum anticancer drugs such as cisplatin, carboplatin and oxaliplatin. 9–11 The activity of organometallic half-sandwich complexes can be tuned by the choice of the arene, chelating and monodentate ligands.…”

Diversity in the Interaction of Amino Acid- and Peptide-Based Hydroxamic Acids with Some Platinum Group Metals in Solution

“…In correlation with these biological roles/effects, hydroxamate-based compounds are frequently used in the design of therapeutics targeting different diseases, like iron overload, cancers, microbial infections, inflammations, etc. [8][9][10][26][27][28][29][30][31][32][33]. A further feature of them is the ability to release NO under certain conditions [12,14].…”