Design, synthesis, and biological investigation of new thiazole-based derivatives as multi-targeted inhibitors endowed with antiproliferative, antioxidant, and antibacterial properties DOI Creative Commons
Hesham A. M. Gomaa,

Asmaa M. Atta,

Mohamed E. Shaker

et al.

Frontiers in Chemistry, Journal Year: 2025, Volume and Issue: 13

Published: May 6, 2025

A novel series of thiazole-based derivatives 11a-f and 12a-f was developed, synthesized, tested for antiproliferative activity as dual EGFR/VEGFR-2 inhibitors, antioxidants, antibacterial agents. The structures the new compounds were validated using NMR spectroscopy elemental microanalysis. against a panel four cancer cell lines MTT assay. Compounds 11d 11f had highest activity, with GI50 values 30 27 nM, respectively, making them more potent than erlotinib (GI50 = 33 nM). Inhibitory studies EGFR VEGFR-2 demonstrated that most inhibitory activity. Furthermore, exhibited significant antioxidant at 10 μM, radical scavenging 71% 73%, compared to reference Trolox (78%). Moreover, exhibit E. coli DNA gyrase, 11b, 11e, 12b displaying efficacy, yielding IC50 182, 190, 197 in comparison novobiocin (IC50 170 11b 11e have efficacy both Gram-positive Gram-negative bacterial strains, by twofold serial dilution experiment. They similar S. aureus, coli, P. aeruginosa, demonstrating potency ciprofloxacin, however reduced effectiveness B. subtilis ciprofloxacin.

Language: Английский

Design, synthesis, and biological investigation of new thiazole-based derivatives as multi-targeted inhibitors endowed with antiproliferative, antioxidant, and antibacterial properties DOI Creative Commons
Hesham A. M. Gomaa,

Asmaa M. Atta,

Mohamed E. Shaker

et al.

Frontiers in Chemistry, Journal Year: 2025, Volume and Issue: 13

Published: May 6, 2025

A novel series of thiazole-based derivatives 11a-f and 12a-f was developed, synthesized, tested for antiproliferative activity as dual EGFR/VEGFR-2 inhibitors, antioxidants, antibacterial agents. The structures the new compounds were validated using NMR spectroscopy elemental microanalysis. against a panel four cancer cell lines MTT assay. Compounds 11d 11f had highest activity, with GI50 values 30 27 nM, respectively, making them more potent than erlotinib (GI50 = 33 nM). Inhibitory studies EGFR VEGFR-2 demonstrated that most inhibitory activity. Furthermore, exhibited significant antioxidant at 10 μM, radical scavenging 71% 73%, compared to reference Trolox (78%). Moreover, exhibit E. coli DNA gyrase, 11b, 11e, 12b displaying efficacy, yielding IC50 182, 190, 197 in comparison novobiocin (IC50 170 11b 11e have efficacy both Gram-positive Gram-negative bacterial strains, by twofold serial dilution experiment. They similar S. aureus, coli, P. aeruginosa, demonstrating potency ciprofloxacin, however reduced effectiveness B. subtilis ciprofloxacin.

Language: Английский

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