engleski

From Design to In vivo Studies of Hybrid Quinazoline-1,3,5-Triazines as Epidermal Growth Factor Receptor (EGFR) Inhibitors

A series of hybrid quinazoline-1, 3, 5-triazine derivatives were synthesized and their activity as EGFR inhibitors was tested using in silico (structure-activity relationship, docking, and molecular dynamics), in vitro (cytotoxicity, EGFR inhibitory activity), in ovo (antiangiogenic activity), and in vivo (effects on body weight, tumor incidence and volume, enzymatic and non-enzymatic antioxidants, biotransformation enzymes, and lipid profile level) methods. The derivatives were found to be active against different cancer and non-toxic against normal cell lines, with some compounds having a very similar profile to erlotinib, a gold standard EGFR inhibitor. The study demonstrated that the best compound (7e) has lead properties against breast cancer and can serve as a starting compound for further development of anti-EGFR compounds with a very different scaffold compared to EGFR inhibitors already present on the market.

EGFR inhibitors ; synthesis ; molecular modelling ; in vitro assays ; in vivo assays

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