This overview's objective was to evaluate the efficacy of benzofuran derivatives, with a focus on phytochemistry and pharmacological applications. The drug's phytochemistry, mechanism of action, pharmacokinetics, pharmacodynamics, and clinical data has all been examined in the pertinent literature. Derivatives of benzofuran have been demonstrated to have positive effects, therefore they have been utilized in many cases in everyday patients; nevertheless, there have also been reports of serious pharmacological side effects. The relevance of the benzofuran moiety has been clarified by a number of biological studies, suggesting that it may be a useful medicinal agent. A thorough pharmacological evaluation and synthesis of benzofuran analogs are given in this review.