Synthesis and antitumour evaluation of mono- and multinuclear [2+1] tricarbonylrhenium(I) complexes

European Journal of Medicinal Chemistry
Dylan GiffardGregory S Smith

Abstract

A series of mono- and multinuclear [2 + 1] Re(I) tricarbonyl complexes were synthesised and evaluated as antiproliferative agents against the epithelial carcinoma (A431), colon carcinoma (DLD-1) and ovarian cancer (A2780) tumour cell lines and a healthy fibroblast (BJ) cell line. The compounds have moderate to good activity against the tumour cell lines, with the trinuclear and tetranuclear complexes showing selective cytotoxicity towards the tumour cell lines. The Re(I) complexes were found to influence programmed cell death mechanisms in vitro. They were able to inhibit the soluble form of the Fas receptor in malignant cells, allowing the Fas domain to receive the apoptotic signal through an extrinsic pathway. The complexes augmented the pro-apoptotic Bax-α concentrations, with the tetranuclear complex more superior at modulating the Bax-α molecular target in all tested cell lines, which influenced its cell growth inhibitory activity. The tetranuclear complex has the best activity against all tumour cell lines.

Citations

Mar 14, 2019·Dalton Transactions : an International Journal of Inorganic Chemistry·Liang HeZong-Wan Mao
Sep 3, 2019·Current Pharmaceutical Design·Philippe ColleryVeena Vijaykumar
Jul 11, 2019·Nucleosides, Nucleotides & Nucleic Acids·Muhammed Bilaal IsmailMatthew Piers Akerman
Aug 9, 2020·Dalton Transactions : an International Journal of Inorganic Chemistry·Zheng-Yin PanLiang He
Jul 8, 2020·Inorganic Chemistry·Sierra C MarkerJustin J Wilson

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