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Updated: Aug 8, 2025
The Synthesis, Characterization and Reactivity of a Series of Ruthenium N-triphosPh Complexes
Published on: April 10, 2015
Anticancer evaluation of new organometallic ruthenium(ii) flavone complexes
Mai Khater1,2, John A Brazier1, Francesca Greco1
1School of Pharmacy, University of Reading Whiteknights Reading RG6 6AD UK f.greco@reading.ac.uk h.m.i.osborn@reading.ac.uk.
Abstract:
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 an 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 MCF-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.
Insights
Ruthenium (Ru) complexation with flavones altered their anticancer properties. While antiangiogenic activity was lost, novel Ru complexes showed enhanced antiproliferative and antimigratory effects on breast cancer cells.
Area of Science:
- Medicinal Chemistry
- Molecular Biology
- Cancer Research
Background:
- Developing single molecules targeting multiple cancer hallmarks like angiogenesis, proliferation, and metastasis is a key strategy for potent anticancer agents.
- Ruthenium (Ru) complexation with bioactive scaffolds can potentially enhance their pharmacological activities.
Purpose of the Study:
- To evaluate the impact of Ruthenium (Ru) chelation on the anticancer activities of two bioactive flavones.
- To investigate the effects of novel Ru complexes on cancer cell proliferation, migration, and angiogenesis.
Main Methods:
- Synthesis and characterization of novel Ruthenium (Ru) complexes (1Ru and 2Ru) with two bioactive flavones (1 and 2).
- In vitro assays including endothelial cell tube formation assay for antiangiogenic activity, antiproliferative assays on MCF-7 and MDA-MB-231 breast cancer cells, and cell migration assays.
- DNA interaction studies using non-intercalative binding with VEGF and c-myc i-motif DNA sequences.
Main Results:
- The novel Ru complexes (1Ru and 2Ru) demonstrated a loss of antiangiogenic activity compared to their parent flavones.
- 1Ru significantly enhanced the antiproliferative and antimigratory activities of flavone 1 on MCF-7 breast cancer cells.
- 2Ru diminished the cytotoxic activity of flavone 2 on MCF-7 and MDA-MB-231 cells but significantly enhanced migration inhibition, particularly on MDA-MB-231 cells.
- Both Ru complexes exhibited non-intercalative interactions with VEGF and c-myc i-motif DNA sequences.
Conclusions:
- Ruthenium (Ru) complexation modulates the pharmacological profile of flavones, leading to varied anticancer effects.
- While antiangiogenic properties were reduced, Ru complexation can enhance antiproliferative and antimigratory activities against specific breast cancer cell lines.
- The findings suggest potential for developing Ru-flavone complexes as targeted anticancer agents, warranting further investigation into their mechanisms of action.
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