Recent advances in antitumor indole-chalcone derivatives: a mini review

Chalcone derivatives, characterized by their α, β-unsaturated ketone structure, represent an important class of compounds with notable anti-cancer and anti-inflammatory properties. Strategic modifications at specific positions of these derivatives have enabled their broad application in treating various types of cancer. The indole group, as a prevalent pharmacophore, also exhibits diverse biological activities including anticancer, anti-inflammatory, and antioxidant effects. Given their complementary properties, the incorporation of indole motif into chalcone scaffolds has emerged as a promising strategy to enhance anticancer efficacy. Recent studies have demonstrated that indole-chalcone derivatives exert potent anticancer effects through various molecular targets, including tubulin, thioredoxin reductase (TrxR), carbonic anhydrase IX (CA IX), and DNA, etc. This review aims to summarize recent advances in the development of indole-chalcone derivatives, examining their diverse structural frameworks and structure-activity relationships. Additionally, we analyzed the molecular targets of these derivatives and explored the application of Proteolysis Targeting Chimera (PROTAC) technology for target identification, with the goal of advancing targeted protein degradation strategies in cancer treatment.