Abstract
Benzofuran compounds are a class of compounds that are ubiquitous in nature. Numerous studies have shown that most benzofuran compounds have strong biological activities such as anti-tumor, antibacterial, anti-oxidative, and anti-viral activities. Owing to these biological activities and potential applications in many aspects, benzofuran compounds have attracted more and more attention of chemical and pharmaceutical researchers worldwide, making these substances potential natural drug lead compounds. For example, the recently discovered novel macrocyclic benzofuran compound has anti-hepatitis C virus activity and is expected to be an effective therapeutic drug for hepatitis C disease; novel scaffold compounds of benzothiophene and benzofuran have been developed and utilized as anticancer agents. Novel methods for constructing benzofuran rings have been discovered in recent years. A complex benzofuran derivative is constructed by a unique free radical cyclization cascade, which is an excellent method for the synthesis of a series of difficult-to-prepare polycyclic benzofuran compounds. Another benzofuran ring constructed by proton quantum tunneling has not only fewer side reactions, but also high yield, which is conducive to the construction of complex benzofuran ring systems. This review summarizes the recent studies on the various aspects of benzofuran derivatives including their important natural product sources, biological activities and drug prospects, and chemical synthesis, as well as the relationship between the bioactivities and structures.
Highlights
A great number of heterocyclic compounds and heterocyclic fragments are present in many drugs due to their versatility and unique physicochemical properties and have become an important basis for medicinal chemistry.[1]
The purpose of this review is to summarize the recently reported natural sources of benzofuran derivatives, the research progress of their biological activities and the synthesis of some common benzofuran compounds, to help readers deeply understand the important roles of benzofurans in medicinal chemistry
This review has highlighted the various aspects of benzofuran derivatives including their important natural product sources, biological activities and drug prospects, and chemical synthesis
Summary
Compounds.[20,21] In addition, some 2-arylbenzofurans derived from natural products have good biological activities,[22] such as anti-cancer,[23] anti-in ammatory,[24] anti-oxidative,[25] and antibacterial activities[26,27] Recently, an oral active and blood–brain barrier permeable benzofuran analog has been found to exhibit potent anti-amyloid aggregation activity, which can provide an alternative treatment for Alzheimer's disease (AD).[28]. The drug can inhibit rapid sodium ion in ux in atrial and myocardial conduction bers, slow down conduction velocity, reduce sinus node autonomy, and has a good effect in dealing with paroxysmal supraventricular tachycardia, atrial premature beats, and premature ventricular contractions. It is mainly used as an antiarrhythmic and anti-angina drug (Fig. 3).[30,31]. Saprophytic ora.[39] Usnic acid has potential anti-tumor activity as well as other biological properties against mitosis and antioxidants.[40,41,42] compounds discovered and isolated from natural animals and plants in recent years (Table 1)
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