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.
 
 KEY WORDS: Synthesis, Nitrogen heterocycles, Carboxamide, Antitumor agents
 
 Bull. Chem. Soc. Ethiop. 2021, 35(2), 449-459.
 DOI: https://dx.doi.org/10.4314/bcse.v35i2.17
Highlights
The rapid spread of cancer has sparked an intense worldwide search for new nitrogen heterocycles containing carboxamide moiety, which may be used in designing novel antitumor drugs
We have described in this paper the synthesis of new nitrogen heterocycles bearing biologically active N-(4-bromophenyl) carboxamide moiety by using diethyl oxalate and pbromoaniline as starting material
The compound 7 was reacted with carbon disulphide in pyridine under reflux gave the corresponding N-(4-bromophenyl)-5-thioxo-1,3,4oxadiazole-2-carboxamide (8)
Summary
The rapid spread of cancer has sparked an intense worldwide search for new nitrogen heterocycles containing carboxamide moiety, which may be used in designing novel antitumor drugs. We have described in this paper the synthesis of new nitrogen heterocycles bearing biologically active N-(4-bromophenyl) carboxamide moiety by using diethyl oxalate and pbromoaniline as starting material. A mixture of benzimidazole-2-carboxamide 4 (0.01 mol) and ethyl chloro acetate (0.01 mol) in dimethyl formamide (30 mL) was heated under reflux for 6 h, cooled and poured into water.
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