De Filippis Barbara, Ammazzalorso Alessandra, Fantacuzzi Marialuigia, Giampietro Letizia, Maccallini Cristina, Amoroso Rosa
Dipartimento di Farmacia, Università "G. d'Annunzio", via dei Vestini 31, 66100, Chieti, Italy.
ChemMedChem. 2017 Apr 20;12(8):558-570. doi: 10.1002/cmdc.201700045. Epub 2017 Mar 28.
Stilbene is an abundant structural scaffold in nature, and stilbene-based compounds have been widely reported for their biological activity. Notably, (E)-resveratrol and its natural stilbene-containing derivatives have been extensively investigated as cardioprotective, potent antioxidant, anti-inflammatory, and anticancer agents. Starting from its potent chemotherapeutic activity against a wide variety of cancers, the stilbene scaffold has been subject to synthetic manipulations with the aim of obtaining new analogues with improved anticancer activity and better bioavailability. Within the last decade, the majority of new synthetic stilbene derivatives have demonstrated significant anticancer activity against a large number of cancer cell lines, depending on the type and position of substituents on the stilbene skeleton. This review focuses on the structure-activity relationship of the key compounds containing a stilbene scaffold and describes how the structural modifications affect their anticancer activity.
芪是自然界中一种丰富的结构骨架,基于芪的化合物因其生物活性已被广泛报道。值得注意的是,(E)-白藜芦醇及其含天然芪的衍生物作为心脏保护剂、强效抗氧化剂、抗炎剂和抗癌剂已被广泛研究。从其对多种癌症的有效化疗活性出发,芪骨架已进行了合成操作,目的是获得具有改善抗癌活性和更好生物利用度的新类似物。在过去十年中,大多数新的合成芪衍生物已显示出对大量癌细胞系具有显著的抗癌活性,这取决于芪骨架上取代基的类型和位置。本综述重点关注含芪骨架关键化合物的构效关系,并描述结构修饰如何影响其抗癌活性。