Synthesis and Biological Evaluation of Chromene-1,3,4-Oxadiazole based 1,2,3-Triazoles: EGFR-targeting Anticancer Agents
K. Vidya
Abstract
Abstract In search of the better anticancer agents, a series of chromene-1,3,4-oxadiazole containing 1,2,3-triazole derivatives were synthesized using 6-fluoro-2-(5-(prop-2-yn-1-ylsulfonyl)-1,3,4-oxadiazol-2-yl)-4H-chromen-4-one and freshly prepared substituted aryl azides. The newly synthesized derivatives were evaluated for their in vitro cytotoxic activity against MCF-7 and A-549. Among all the synthesized compounds, 6-fluoro-2-(5-(((1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-4H-chromen-4-one and 2-(5-(((1-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-one shows potent anticancer activity as compared to remaining derivatives. Similarly, the compounds 2-(5-(((1-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-one and 2-(5-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-ones were found to be active against EGFR.