Issue 33, 2024

The role of stereochemistry in the anticancer activity of Re(i) tricarbonyl complexes

Abstract

Cancer is a leading cause of death worldwide, accounting for about one among six deaths, so the quest for new and improved therapies is of crucial importance. The discovery of cisplatin as an anticancer agent has paved the way for the development of other metal-based therapeutic agents and Re(I)-based candidates have been recently found to show promising results. It is known as well that chirality plays a central role in the interactions of metal-based drugs with intrinsically chiral biomolecules such as membrane transport proteins or DNA. To further exploit this property, we have developed a series of diastereomeric dinuclear Re(I) complexes with chiral ligands containing pinene-bipyridine units. These complexes offer unique insights into the relation between stereochemistry and biological activity. Single-crystal X-ray diffraction studies, spectroscopic analysis, including UV-Vis and circular dichroism (CD), confirmed the chiral structures of these complexes. Biological activity assessments were carried out against various cancer cell lines, with a particular focus on breast and colon cancer. The diastereomers exhibited distinct anticancer activities, with some displaying promising results. Notably, one diastereomer showed exceptional cytotoxicity against HCT116 and MCF-7 cancer cells. This research underscores the significance of chirality in the design of novel anticancer agents, providing insights into the potential of dinuclear Re(I) complexes as effective candidates for cancer treatment.

Graphical abstract: The role of stereochemistry in the anticancer activity of Re(i) tricarbonyl complexes

Supplementary files

Article information

Article type
Paper
Submitted
05 Jun 2024
Accepted
05 Jul 2024
First published
12 Jul 2024
This article is Open Access
Creative Commons BY license

Dalton Trans., 2024,53, 13743-13755

The role of stereochemistry in the anticancer activity of Re(I) tricarbonyl complexes

A. B. Solea, G. Demirci, F. M. Harvey, A. Crochet, F. Zobi and O. Mamula Steiner, Dalton Trans., 2024, 53, 13743 DOI: 10.1039/D4DT01643B

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