AI Article Synopsis
- Third-generation aromatase inhibitors like anastrozole and letrozole are important for treating ER+ breast cancers in postmenopausal women, and researching their metal coordination properties could help develop new cancer drugs.
- A new ruthenium(II) arene complex incorporating anastrozole was synthesized and showed promising results, being the most stable in cell media and demonstrating high cellular uptake and cytotoxic effects on specific breast cancer cell lines.
- This complex also reduced aromatase activity in certain cells and was not toxic to zebrafish embryos, suggesting it could be a good candidate for further research in cancer treatment.
Article Abstract
Third-generation aromatase inhibitors such as anastrozole (ATZ) and letrozole (LTZ) are widely used to treat estrogen receptor-positive ER+ breast cancers in postmenopausal women. Investigating their ability to coordinate metals could lead to the emergence of a new category of anticancer drug candidates with a broader spectrum of pharmacological activities. In this study, a series of ruthenium (II) arene complexes bearing the aromatase inhibitor anastrozole was synthesized and characterized. Among these complexes, [Ru( CH)(PPh)( ATZ)Cl]BPh () was found to be the most stable in cell culture media, to lead to the highest cellular uptake and cytotoxicity in two ER+ human breast cancer cell lines (MCF7 and T47D), and to induce a decrease in aromatase activity in H295R cells. Exposure of zebrafish embryos to complex (12.5 μM) did not lead to noticeable signs of toxicity over 96 h, making it a suitable candidate for further investigations.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6874409 | PMC |
| http://dx.doi.org/10.1021/acs.organomet.8b00897 | DOI Listing |
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