Synthesis and biological evaluation of pyrido[3,2,1-ij][1,2,3]triazolo[4,5-c] quinolinones: PEG-400 mediated one-pot reaction under ultrasonic irradiation

A general strategy was developed for the synthesis of fused pyrido[3,2,1-ij] [1-3]triazolo[4,5-c]quinolinones from 1-(3-iodoprop-2-yn-1-yl)-4-methylquinolin-2(1H)-one and several azides using ultrasound irradiation in PEG-400 medium. In vitro anticancer activity of all these derivatives against MCF-7 (breast) and A-549 (alveolar carcinoma) cancer cell lines using the MTT assay. Among all the tested compounds, 4e, 4f, and 4j displayed remarkable cytotoxic activity against both cancer cell lines as compared to the remaining compounds. In specific, compound 4f showed superior activity against A-549 cell lines than the standard drug Erlotinib. Later, the results of inhibitory assay of potent compounds 4e, 4f, and 4j against the tyrosine kinase epidermal growth factor receptor (EGFR) revealed that compound 4f shows equipotent activity of the reference drug erlotinib.

Automated summary

A general strategy for the synthesis of fused pyrido[3,2,1-ij][1-3]triazolo[4,5-c]quinolinones was developed using ultrasound irradiation in PEG-400 medium. The anticancer activity of these derivatives against MCF-7 and A-549 cell lines was evaluated using the MTT assay. Compounds 4e, 4f, and 4j showed remarkable cytotoxic activity against both cancer cell lines, with 4f exhibiting superior activity against A-549 cells compared to the standard drug Erlotinib. Inhibitory assay results revealed that compound 4f has equipotent activity against EGFR.