Anticancer evaluation of new organometallic ruthenium(II) flavone complexes

Khater, M., Brazier, J. ORCID: https://orcid.org/0000-0002-4952-584X, Greco, F. and Osborn, H. ORCID: https://orcid.org/0000-0002-0683-0457 (2023) Anticancer evaluation of new organometallic ruthenium(II) flavone complexes. Medicinal Chemistry, 14 (2). pp. 253-267. ISSN 2632-8682 doi: 10.1039/D2MD00304J

Abstract/Summary

Targeting multiple malignancy features such as angiogenesis, proliferation and metastasis with one molecule is an effective strategy in developing potent anticancer agents. Ruthenium metal complexation to bioactive scaffolds is reported to enhance their biological activities. Herein, we evaluate the impact of Ru chelation on the pharmacological activities of two bioactive flavones (1 and 2) as anticancer candidates. The novel Ru complexes (1Ru and 2Ru) caused a loss of their parent molecules’ antiangiogenic activities in endothelial cell tube formation assay. 1Ru enhanced the antiproliferative and antimigratory activities of its 4-oxoflavone 1 on MCF-7 breast cancer cells (IC50 = 66.15 ± 5 µM and 50% migration inhibition, p < 0.01 at 1 µM). 2Ru diminished 4-thioflavone’s (2) cytotoxic activity on MF-7 and MDA-MB-231 yet significantly enhanced 2’s migration inhibition (p < 0.05) particularly on the MDA-MB-231 cell line. The test derivatives also showed non-intercalative interaction with VEGF and c-myc i-motif DNA sequences.

Item Type	Article
URI	https://reading-clone.eprints-hosting.org/id/eprint/109188
Identification Number/DOI	10.1039/D2MD00304J
Refereed	Yes
Divisions	Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Medicinal Chemistry Research Group
Publisher	Royal Society of Chemistry
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