Synthesis and biological evaluation of 4-(1H-imidazol-2-yl)-2-(pyrimidin-5-yl)oxazoles as potent anticancer agents

Abstract

A new series of aryl derivatives of 4-(1H-imidazol-2-yl)-2-(pyrimidin-5-yl)oxazoles 11a–j were synthesised and their structures were characterized by analytical techniques. Further, the biological applications of the newly prepared compounds 11a–j were evaluated against four human cancer cell lines including breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205) and ovarian cancer (A2780), using the standard MTT assay, with etoposide as the positive control. The obtained results showed that most of the tested compounds displayed more potent activity with IC50 values range from 0.01 ± 0.098 µM to 8.12 ± 5.69 µM, whereas the positive control showed IC50 values ranging from 0.17 ± 0.034 µM to 3.34 ± 0.152 µM. Among them, five compounds 11a, 11b, 11c, 11d and 11e possessed more potent activity. In which, one compound 11a, showed superior anticancer activity.

Keywords

• Suzuki-coupling
• Imidazole
• Oxazole
• Pyrimidine
• Anticancer activity