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

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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Publication Details

Journal
Future Medicinal Chemistry
Published
2026-01-26
DOI
https://doi.org/10.1080/17568919.2026.2617612
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
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article

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

Fisnik Laha, Demokrat Nuha, Asaf Evrim Evren, Arbëri Bytyçi et al.
Future Medicinal Chemistry
Synthesis and biological activity
article

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

Fisnik Laha, Demokrat Nuha, Asaf Evrim Evren, Arbëri Bytyçi, Pajtim Bytyçi, Erinda Lika, Osman Fetosh, Simone Carradori
article en

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.

Future Medicinal ChemistryVol. 18(4)
Agricultural University of Tirana (AL), Anadolu University (TR), University of Chieti-Pescara (IT), University for Business and Technology (XK), EYDAP (Greece) (GR)
Good health and well-being
Openalex Percentile: Top 76%
Synthesis and biological activity
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