Romanian Society of Pharmaceutical Sciences

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IN VITRO PROSPECTION OF ANTICANCER ACTIVITY OF SOME BROMINATED DERIVATIVES WITH ACETOPHENONE SCAFFOLD

ANA-MARIA ZBANCIOC *, ALEXANDRU VASINCU, ANCA MIRON, GABRIELA TATARINGA

1University of Medicine and Pharmacy “Grigore T. Popa” Iași, Romania

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A series of brominated acetophenone derivatives, previously synthesised, were cytotoxic evaluated against different tumour human cell lines: breast adenocarcinoma MCF7, alveolar adenocarcinoma A549, colorectal adenocarcinoma Caco2 and prostate adenocarcinoma PC3 by a colorimetric assay, using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT assay). It was also studied the effect of these compounds (5a-e) on the viability of human normal breast epithelial cells MCF12F (non-tumorigenic breast epithelial cell line). Considering the fact that the pro-oxidant potential can explain, at least partially, a selective antitumor action, the pro-oxidant effects of the brominated derivatives 5a-e in MCF7, A549, Caco2 and PC3 tumour cells were also evaluated. The results showed that the most active compound was 5c which exhibited remarkable cytotoxicity against all tested tumour cell lines, with IC50 values of 11.80 ± 0.89 μg/mL, in alveolar adenocarcinoma A549 cells, 18.40 ± 4.70 μg/mL, in colorectal adenocarcinoma Caco2 cells and IC50 < 10 μg/mL, in breast adenocarcinoma MCF7 cells and in prostate adenocarcinoma PC3 cells. Against the normal, breast epithelial cell line MCF12F derivative 5c showed the lowest cytotoxicity (IC50 ˃ 100 μg/mL 10.77 ± 2.14%). Brominated derivatives 5d and 5e showed good pro-oxidant activity against A549 cells (52.26 ± 3.12% and 69.62 ± 4.13%, respectively) and Caco2 (67.89 ± 2.17% and respectively, 58.89 ± 3.11%).