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.

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苯并呋喃衍生物与潜在抗癌活性的构效关系。

苯并呋喃是一种天然存在于植物中的杂环化合物，也可以通过合成反应获得。多种物化特性和多用途特性区分苯并呋喃，其化学结构由稠合苯环和呋喃环组成。苯并呋喃衍生物是必不可少的化合物，具有重要的生物活性，可以设计出与传统疗法相比具有更高功效的新型疗法。因此，药物化学家利用其核心合成了可应用于多种疾病的新衍生物。苯并呋喃在高血压、神经退行性和氧化性病症以及血脂异常等慢性疾病中表现出潜在的疗效。在急性感染中，苯并呋喃显示出对病毒、细菌和寄生虫等微生物的抗感染特性。近年来，获得性或耐药性癌症病例的复杂性和数量大幅增加。苯并呋喃衍生物显示出潜在的抗癌活性，在化疗期间通常遇到的不良事件的发生率或严重程度较低。本综述讨论了几种苯并呋喃衍生物的构效关系 (SAR)，以阐明高效和选择性抗癌活性的可能替代选择和结构要求。