Thio-Coumarin-Chalcone Hybrids as Promising Therapeutic Agents: A Review of Synthesis and Biological Evaluation

The construction of new medicinal agents by molecular hybridization strategies is a powerful and emerging medicinal chemistry strategy to make novel medicinal agents with unique mechanisms of action through current discovery and development. Molecular hybridization is an important strategy in medicinal chemistry that can be effectively utilized to design multifunctional molecules through the combination of varied pharmacophores to obtain synergistic or additive effects. In this review, we analyze the synthesis and biological evaluation of a new class of hybrid Thio coumarin-chalcone derivatives. Thio coumarins are well-established preferred scaffolds with a wide array of biological activities. Chalcones are an additional α,β-unsaturated ketone system which is well known for its anticancer, antifungal, antimicrobial and anti-inflammatory properties. Similarly, the conjugation of these two bioactive molecules seems to be a promising approach to design and synthesise new molecules with better efficacy and high potential to overcome existing resistance. This review highlights on the synthetic methodologies utilized for the synthesis of hybrid scaffold, particularly for the synthesis of coumarin–chalcon precursors and Claisen Schmidt condensation for hybrid molecules. Additionally, it outlines the in vitro activities of these derivatives against a range of diseases and also highlights pertinent SAR findings. The discussion goes on to the possible mechanisms of action such as interfering with signaling pathways and biofilm inhibition that highlight the potential of Thio coumarin-chalcone derivatives-as next-generation antimicrobials.