Isoxazole derivatives are nitrogen and oxygen containing heterocycles exhibiting diverse pharmacological activities. They represent a significant group of five-membered compounds have been studied in medicinal chemistry due to their extensive range of biological activities and beneficial pharmacological characteristics. The adjacency of nitrogen and oxygen atoms within the aromatic structure provides unique electronic properties, allowing for strong interactions with various biological targets. Recent developments in synthetic techniques, including microwave-assisted synthesis, cyclization reactions, multicomponent reactions, and environmentally friendly chemistry methods, have accelerated the rapid creation of structurally varied isoxazole derivatives. Various isoxazole derivatives have demonstrated significant biological activities. Several compounds exhibited potent inhibitory activity against various cancer cell lines such as MCF-7, HeLa, A549 and HepG2.The structure-activity relationship studies revealed that electron-withdrawing substituents including chloro, fluoro and nitro groups generally enhance biological activity. This review highlights recent advancements in both the chemistry and pharmacological uses of isoxazole-based compounds, focusing particularly on their anticancer, antimicrobial, and antifungal properties. Special emphasis is placed on hybrid molecules featuring isoxazole connected to pharmacologically active frameworks such as pyrazole, chalcone, quinoline, and thiazole. These hybrid systems have shown improved biological activity.
L.* et al. (2026) studied this question.