Abstract

SYNTHESIS AND BIOLOGICAL EVALUATION OF NEWER BENZOFURAN DERIVATIVES AS POTENTIAL ANTICANCER AND ANTHELMINTIC AGENTS

Rohit Kumar Saxena*, Prashant Kumar and Shruti Varshney

Abstract

In the present study we have made an attempt to synthesize novel benzofuran derivatives and evaluate them as potential therapeutic agents by anticancer screening. First, 2-ethoxy carbomethoxy (1) was prepared from 2-hydroxy acetophenone and ethylchloroacetate, which gave ethyl-3-methyl-2-benzofuran carboxylate (2) on reaction with anhydrous potassium carbonate. Treatment of ethyl-3-methyl-2- benzofuran carboxylate (2) with hydrazine hydrate afforded 3-methyl- 2-benzofuran carbohydrazide (3) and then Condensation of 3-methyl- 2-benzofuran carbohydrazide (4) with various substituted benzaldehydes led to a novel series of benzofuran derivatives (5a-k). The synthesized compounds were analyzed by physical and analytical data. The synthesized compounds were evaluated for their short-term anticancer activity. The synthesized imidazole derivative possessed significant cytotoxic activity against Ehrlich’s Ascites Carcinoma (EAC) cell lines and HEP2 cell line by SRB assay. The synthesized compounds have shown moderate to good anthelmintic activity.

Keywords: Benzofuran. Schiff’s base. Anticancer activity. Anthelmintic activity.