Abstract
In this research paper, we report the cytotoxic and apoptotic effects of 1,2,3-triazole derivatives in a unique 7a–g or hybrid form with isoxazoline 8a–g using the eugenol as a precursor in HT-1080 fibrosarcoma, MCF-7, and MDA-MB-231 breast carcinoma, and A-549 lung carcinoma. Data obtained on the cytotoxic effects have shown that hybrid compounds 8a–e induced a significant anticancer activity and are more important than the ones of 1,2,3-triazole derivatives 7a–g with IC50 ranging from 18 to 43 μM for the hybrids 8a–e and from 15 to 29 μM for mono-adducts 7a–g in all cell lines. Concerning the apoptotic study, compounds 7b and 8a can induce apoptosis in HT-1080 and A-549 cells as revealed by Annexin-V labeling and caspase-3/7 activity, also, the apoptotic effect was accompanied by cell cycle arrest at G2/M phase in the case of compounds 7b and 8a. Both compounds were evaluated in-silico through molecular docking and molecular dynamics and compound 8a is very active against Bcl-2 protein triggering apoptosis phenomenon by intrinsic pathway, therefore compound 8a is a potential candidate to inhibit the anti-apoptotic protein (Bcl-2).
Communicated by Ramaswamy H. Sarma.
Disclosure statement
No potential conflict of interest was reported by the authors.
Data availability statement
The authors confirm that the data supporting the findings of this study are available within the article and its supplementary materials.