Ruthenium(II)-Arene Thiocarboxylates: Identification of a Stable Dimer Selectively Cytotoxic to Invasive Breast Cancer Cells.

Ruthenium(II)-Arene Thiocarboxylates: Identification of a Stable Dimer Selectively Cytotoxic to Invasive Breast Cancer Cells.
Chembiochem. 2019 Nov 08;:
Authors: Stephens L, Levina A, Trinh I, Blair V, Werrett M, Lay P, Andrews P
Abstract
Ru(II)-arene complexes provide a versatile scaffold for novel anti-cancer drugs. A new series of Ru(II)-arene-thiocarboxylato dimers 1-7 were synthesized and characterized. Three of the complexes (2a,b and 5) showed promising anti-proliferative activities in MDA-MB-231 (human invasive breast cancer) cells, and were further tested in a panel of fifteen cancerous and non-cancerous cell lines. Complex 5 showed moderate but remarkably selective activity in MDA-MB-231 cells (IC50 = 39 ± 4 mM Ru). Real-time proliferation studies showed that 5 induced apoptosis in MDA-MB-231 cells but had no effect in A549 (human lung cancer, epithelial) cells. By contrast, 2a and b showed moderate anti-proliferative activity, but no apoptosis, in either cell line. Selective cytotoxicity of 5 in aggressive, mesenchymal-like MDA-MB-231 cells over many common epithelial cancer cell lines (including non-invasive breast cancer MCF-7) makes it an attractive lead compound for the development of specifically anti-metastatic Ru complexes with low systemic toxicity.
PMID: 31701616 [PubMed - as supplied by publisher]

Source: Chembiochem - November 7, 2019 Category: Biochemistry Authors: Stephens L, Levina A, Trinh I, Blair V, Werrett M, Lay P, Andrews P Tags: Chembiochem Source Type: research