Synthesis, characterization and biological evaluation of some 2-arylbenzoxazole acetic acid derivatives as potential anticancer agents

Abstract

A series of 2-arylbenzoxazole compounds possessing a cytotoxic activity as potential anticancer agents has been synthesised. Oxidative coupling of benzaldehyde with o-aminophenol utilizing lead tetraacetate approach has been used to realize the synthesis of compounds 1-11. The cytotoxicity of 1-11 have been screened against breast cancer cell line MCF-7 and human colon cancer cell line HCT-116 utilizing doxorubicin as reference drug. Among these compounds, 2-(3-benzyloxyphenyl)benzoxazole-5-acetic acid 5 and 2-(4-methoxyphenyl)benzoxazol-5-acetic acid 10, are found to be promising cytotoxic compounds against MCF-7 cell line. In addition, this study shows that the presence of acetic acid group at position 5 of benzoxazole nucleus enhances the activity. Moreover, it is noticed that the presence of oxygen atom directly linked to the phenyl substituent improves activity. The results offer a new benzoxazole based template to design and develop novel antineoplastic agents.