Synthesis of novel nitrogen heterocycles bearing biological active carboxamide moiety as potential antitumor agents

Abstract

ABSTRACT. In the present study, synthesis of a simple series of nitrogen heterocycles containing N-(p-bromophenyl) carboxamide moiety, such as benzimidazole, benzoxazine, oxadiazole and triazole compounds, by using 4-bromo aniline and diethyl oxalate as a key starting material has been described. Five nitrogen heterocycles compounds moiety were evaluated for their anticancer activity against MCF-7 cell line. The results revealed that compound 8 (N-(4-bromophenyl)-5-thioxo-1,3,4-oxadiazole-2-carboxamide) was the most potent cytotoxic activity. Cell cycle analysis demonstrated that compound 8 induce cell cycle arrest at G1 phase with apoptosis inducing activity marked by increase in G0 phase. \n\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0\xa0 \nKEY WORDS: Synthesis, Nitrogen heterocycles, Carboxamide, Antitumor agents \n\xa0 \nBull. Chem. Soc. Ethiop. 2021, 35(2), 449-459. \nDOI: https://dx.doi.org/10.4314/bcse.v35i2.17