Thiosemicarbazone Derivatives as Promising Therapeutic Agents: Recent Advances and Biological Applications

Objective: Thiosemicarbazones are an important class of sulfur and nitrogen-containing Schiff base derivatives that have attracted huge attention because of their diverse pharmacological properties. Structural flexibility, strong metal-chelating ability, and tunable electronic properties make them promising scaffolds in the fields of medicinal and bioinorganic chemistry. The objective of this review is to give an overview of the recent developments in substituted thiosemicarbazones with special emphasis on phenyl-substituted thiosemicarbazones. This review also includes other substituents of thiosemicarbazones and covers articles from 1993-2025. Methods: This review was designed as a narrative literature review to summarize and critically discuss the recent developments in thiosemicarbazone (TSC) derivatives, with particular emphasis on their synthesis, coordination chemistry, biological activities, and therapeutic potential. The objective was to provide a comprehensive overview of current research trends and highlight the progress made in the development of biologically active thiosemicarbazone derivatives and their metal complexes Results: Reviews have demonstrated that thiosemicarbazones and their metal complexes exhibit a broad range of biological activities, including anticancer, antimicrobial, antiviral, antifungal, antitubercular, antimalarial, antioxidant, and anti-inflammatory effects. Coordination with transition metals often enhances their biological efficacy by increasing lipophilicity, improving membrane permeability, and facilitating better interaction with biological targets. Additionally, metal complexes may promote redox processes and the generation of reactive oxygen species, contributing to their therapeutic potential. Discussion: The biological activities of thiosemicarbazones are strongly influenced by variations in structure, including ligand substitution patterns, electronic properties, and the nature of the coordinated metal ion. Conclusion: Overall, thiosemicarbazones are organic compounds that represent versatile bioactive scaffolds with significant potential for the design and development of novel therapeutic agents.