Prenylated flavonoids, a unique class of flavonoids which combine a flavonoid skeleton and a lipophilic prenyl side-chain, possess great potential biological activities including cytotoxicity, anti-inflammation, anti-Alzheimer, anti-microbial, anti-oxidant, anti-diabetes, estrogenic, vasorelaxant and enzyme inhibition. Recently, prenylated flavonoids have become an indispensable anchor for the development of new therapeutic agents, and have received increasing from medicinal chemists. The prenylated flavonoids have been outstanding developed through isolation, semi or fully synthesis in a very short period of time, which proves the great value in medicinal chemistry researches. In this review, research progress of prenylated flavonoids including natural prenylated flavonoids, structural modification, synthetic methodologies and pharmacological activities was summarized comprehensively. Furthermore, the structure–activity relationships (SARs) of prenylated flavonoids were summarized which provided a basis for the selective design and optimization of multifunctional prenylated flavonoid derivatives for the treatment of multi-factorial diseases in clinic.

异戊二烯化黄酮是一类独特的黄酮类化合物，结合了黄酮骨架和亲脂性异戊二烯侧链，具有巨大的潜在生物活性，包括细胞毒性、抗炎、抗阿尔茨海默病、抗微生物、抗氧化、抗糖尿病、雌激素、血管舒张剂和酶抑制作用。近来，异戊二烯化黄酮类化合物已成为开发新治疗剂不可或缺的基础，并越来越受到药物化学家的关注。异戊二烯化黄酮在很短的时间内通过分离、半合成或全合成得到了突出的发展，证明了其在药物化学研究中的巨大价值。本文综述了异戊二烯化黄酮的研究进展，包括天然异戊二烯化黄酮、结构修饰、综合总结了合成方法和药理活性。此外，总结了异戊二烯化黄酮类化合物的构效关系（SARs），为临床上用于治疗多因素疾病的多功能异戊二烯化黄酮衍生物的选择性设计和优化提供了基础。