Department of General Medicine, Sher-I-Kashmir Institute of Medical Sciences (SKIMS), Srinagar, Jammu and Kashmir, 190001, India.
Pharmaceutical Chemistry Division, Chandigarh College of Pharmacy, Landran, Punjab-140301, India.
Anticancer Agents Med Chem. 2022;22(20):3343-3369. doi: 10.2174/1871520622666220421094055.
Flavonoids, a class of polyphenolic secondary metabolites, are present in fruits, vegetables, beverages such as wine and tea abundantly. Flavonoids exhibit a diverse array of pharmacological activities, including anticancer activity, and are toxic to cancer cells but not harmful to healthy cells. Besides, humans and animals cannot synthesize flavonoids, which leads to a dramatic increase in the consumption of plant flavonoids. Flavonoids consist of a 15- carbon skeleton in C6-C3-C6 rings with divergent substitution patterns to form a series of compounds. Due to their multi-faceted mechanism of action by modulating various signaling pathways associated with apoptosis, cellular proliferation, inflammation, differentiation, metastasis, angiogenesis, they interrupt the initiation, promotion, and progression of cancer. The present review highlights the Structural Activity Relationship (SAR) of flavonoids and recent insights on the progress of natural flavonoids and their synthetic analogs as prospective drug candidates against cancer, along with molecular mechanisms of action.
类黄酮是一类多酚类次生代谢产物，广泛存在于水果、蔬菜、葡萄酒和茶等饮料中。类黄酮具有多种药理活性，包括抗癌活性，对癌细胞有毒但对健康细胞无害。此外，人类和动物不能合成类黄酮，这导致植物类黄酮的摄入量大幅增加。类黄酮由 C6-C3-C6 环的 15 个碳原子骨架组成，具有不同的取代模式，形成一系列化合物。由于它们通过调节与细胞凋亡、细胞增殖、炎症、分化、转移、血管生成相关的各种信号通路的多方面作用机制，它们中断了癌症的起始、促进和进展。本综述强调了类黄酮的结构活性关系（SAR），以及天然类黄酮及其合成类似物作为抗癌候选药物的最新进展，以及作用机制的分子机制。
