Structure–Activity Relationship of Benzofuran Derivatives with Potential Anticancer Activity

SIMPLE SUMMARY: Cancer is the leading cause of death worldwide and responsible for killing approximately 10 million people per year. Fused heterocyclic ring systems such as benzofuran have emerged as important scaffolds with many biological properties. Furthermore, derivatives of benzofurans demonstrate a wide range of biological and pharmacological activities, including anticancer properties. The main aim of this review is to highlight and discuss the contribution of benzofuran derivatives as anticancer agents by considering and discussing the chemical structure of 20 different compounds. Evaluating the chemical structure of these compounds will guide future medicinal chemists in designing new drugs for cancer therapy that might give excellent results in in vivo/in vitro applications. ABSTRACT: Benzofuran is a heterocyclic compound found naturally in plants and it can also be obtained through synthetic reactions. Multiple physicochemical characteristics and versatile features distinguish benzofuran, and its chemical structure is composed of fused benzene and furan rings. Benzofuran derivatives are essential compounds that hold vital biological activities to design novel therapies with enhanced efficacy compared to conventional treatments. Therefore, medicinal chemists used its core to synthesize new derivatives that can be applied to a variety of disorders. Benzofuran exhibited potential effectiveness in chronic diseases such as hypertension, neurodegenerative and oxidative conditions, and dyslipidemia. In acute infections, benzofuran revealed anti-infective properties against microorganisms like viruses, bacteria, and parasites. In recent years, the complex nature and the number of acquired or resistant cancer cases have been largely increasing. Benzofuran derivatives revealed potential anticancer activity with lower incidence or severity of adverse events normally encountered during chemotherapeutic treatments. This review discusses the structure–activity relationship (SAR) of several benzofuran derivatives in order to elucidate the possible substitution alternatives and structural requirements for a highly potent and selective anticancer activity.