Anticancer Activity of Stilbene‐Based Derivatives

• Published in: ChemMedChem Vol. 12; no. 8; pp. 558 - 570
• Main Authors: De Filippis, Barbara, Ammazzalorso, Alessandra, Fantacuzzi, Marialuigia, Giampietro, Letizia, Maccallini, Cristina, Amoroso, Rosa
• Format: Journal Article
• Language: English
• Published: Germany Wiley Subscription Services, Inc 20.04.2017
• Subjects: Angiogenesis Inhibitors - chemistry; Angiogenesis Inhibitors - pharmacology; anticancer agents; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; antiproliferation; Apoptosis - drug effects; Berries; Bioavailability; Cancer; Cell Line, Tumor; Cyclooxygenase 2 Inhibitors - chemistry; Cyclooxygenase 2 Inhibitors - pharmacology; Humans; Isomerism; resveratrol; stilbene analogues; Stilbenes - chemistry; Stilbenes - pharmacology; Structure-Activity Relationship; stilbene analogues; antiproliferation; resveratrol; anticancer agents
• ISSN: 1860-7179; 1860-7187; 1860-7187
• DOI: 10.1002/cmdc.201700045

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. A key scaffold: Stilbene‐based compounds have been described for their cardioprotective, antioxidant, anti‐inflammatory, and anticancer activity. New synthetic stilbene derivatives that show good bioavailability and significant activity against a large number of cancer cell lines have been reported, depending on the type and position of substituents on the stilbene skeleton. This review focuses on the structure–activity relationships of key compounds with a stilbene scaffold and describes how structural modifications affect their anticancer activity.