1. Synthesis and antitumour evaluation of mono- and multinuclear [2+1] tricarbonylrhenium(I) complexes.
- Author
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Giffard, Dylan, Fischer-Fodor, Eva, Vlad, Catalin, Achimas-Cadariu, Patriciu, and Smith, Gregory S.
- Subjects
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ANTINEOPLASTIC agents , *RHENIUM , *METAL complexes , *INORGANIC synthesis , *FIBROBLASTS - Abstract
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. Graphical abstract Image 1 Highlights • Mono- and multinuclear [2 + 1] Re(I) tricarbonyl complexes have been prepared. • The complexes were characterised using several spectroscopic and analytical techniques. • The complexes were evaluated as antiproliferative agents against A431, DLD-1 and A270 tumour cell lines. • The Re(I) complexes all influence programmed cell death mechanisms. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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