Thiazole scaffolds occupy a prominent position in medicinal chemistry due to their electronic diversity and structural adaptability, enabling interaction with multiple biological targets. Over the last decade, these heterocyclic frameworks have received extensive attention for the development of new anticancer and antimicrobial agents. The five-membered thiazole ring, containing both nitrogen and sulfur atoms, provides remarkable chemical stability and versatility, allowing fine-tuning of pharmacological responses. Numerous derivatives have demonstrated significant biological activities, including inhibition of resistant microbial strains and selective cytotoxicity toward tumor cells. This review critically summarizes research published between 2015 and 2025, emphasizing how structural variations within thiazole derivatives influence their biological profiles. A focused discussion on structure - activity relationships (SAR) highlights the influence of electronic, steric, and lipophilic features on potency and selectivity. Integrating both experimental findings and computational insights, the review offers a coherent understanding of how structural modifications govern biological outcomes. Although available pharmacokinetic and toxicity data remain limited, they are identified as important directions for further research. Molecular docking observations are included to illustrate possible interaction modes rather than to define mechanisms. Overall, this work provides an integrative perspective that may guide the rational design of future thiazole-based molecules with improved efficacy and safety.

Thiazole scaffolds as anticancer and antimicrobial agents: recent advances in medicinal chemistry

Carradori, Simone;
2026-01-01

Abstract

Thiazole scaffolds occupy a prominent position in medicinal chemistry due to their electronic diversity and structural adaptability, enabling interaction with multiple biological targets. Over the last decade, these heterocyclic frameworks have received extensive attention for the development of new anticancer and antimicrobial agents. The five-membered thiazole ring, containing both nitrogen and sulfur atoms, provides remarkable chemical stability and versatility, allowing fine-tuning of pharmacological responses. Numerous derivatives have demonstrated significant biological activities, including inhibition of resistant microbial strains and selective cytotoxicity toward tumor cells. This review critically summarizes research published between 2015 and 2025, emphasizing how structural variations within thiazole derivatives influence their biological profiles. A focused discussion on structure - activity relationships (SAR) highlights the influence of electronic, steric, and lipophilic features on potency and selectivity. Integrating both experimental findings and computational insights, the review offers a coherent understanding of how structural modifications govern biological outcomes. Although available pharmacokinetic and toxicity data remain limited, they are identified as important directions for further research. Molecular docking observations are included to illustrate possible interaction modes rather than to define mechanisms. Overall, this work provides an integrative perspective that may guide the rational design of future thiazole-based molecules with improved efficacy and safety.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/873713
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