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Coumarin-Augmented Thiazole Hybrids as Dual Anticancer and Antibacterial Agents.


ABSTRACT: Coumarins are a privileged scaffold in medicinal chemistry, renowned for diverse therapeutic activities including antiviral, anticancer, and neuroprotective effects. Building on our previous work with 3-substituted coumarins as inhibitors of tumor-associated carbonic anhydrases, we report a novel series of thiazol-hydrazono-coumarins targeting the ATP-binding domain of topoisomerase enzymes. Seventeen compounds were synthesized and evaluated for selective cytotoxicity against HeLa cells versus WI-38 fibroblasts and for antimicrobial activity against four ESKAPE pathogens, Escherichia coli, and Salmonella typhimurium. Several derivatives showed potent antibacterial activity, with MICs as low as 0.12 μg/mL against resistant Staphylococcus aureus strains and inhibition zones up to 33 mm again

SUBMITTER: Matar IK 

PROVIDER: S-EPMC12923669 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature