Synthesis, characterization and biological evaluation of newly designed silver(I)-N-heterocyclic carbene (NHC) complexes
Year: 2026
Type: article
Abstract: In this study, we present the design, synthesis, characterization and biological evaluation of novel silver(I)-N-heterocyclic carbene (NHC) complexes as potential chemotherapeutic agents for breast cancer treatment. We assessed their cytotoxicity against breast cancer cell lines with distinct hormone receptor profiles, specifically T47D, MCF-7, and the triple-negative MDA-MB-231. Among these, the ER positive (ER+) cell lines exhibited different results: T47D cells were the most sensitive to all the tested compounds with IC50 values ranging between 6.193 and 10.85 µM, while MCF-7 cells were the most resistant (with IC50 values ranging between 18.35-56.25 µM). The ER negative (ER-) cell line MDA-MB-231 exhibited reduced responsiveness (IC50 of 13.94-27.45 µM), highlighting the clinical challenges associated with triple-negative breast cancers. All the tested compounds were more active against cancer cells than Cisplatin. Notably, complex 2, which features a simple benzyl group ligand, demonstrated the strongest cytotoxic activity, with IC₅₀ values of 6.193 ± 0.18 µM in T47D cells, also the selectivity index (SI) values were consistently higher in T47D cells compared to MCF-7, reflecting the behavior of our reference chemotherapeutic agent, Cisplatin. Flow cytometry confirmed that apoptosis was the predominant mode of cell death, particularly in ER+ cells with the pro-apoptotic effect being most pronounced (50.30% and 29.75%, apoptotic pattern respectively in MCF-7 and T47D cells). Fluorescence microscopy images obtained through AO/PI co-staining revealed also a significant population of apoptotic cells in the ER+ cell lines MCF-7 and T47D. Finally, as potential drugs, these complexes showed promising ADMET scores.
Source: Results in Chemistry
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,870
OpenAlex ID: W7162119645
