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    Synthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studies
    (Wiley, 2023) Kurt, Belma Zengin; Altundag, Ozlem; Tokgoz, Merve Nur; Civelek, Dilek Ozturk; Tuncay, Fulya Oz; Cakmak, Ummuhan; Kolcuoglu, Yakup
    Totally 15 novel flurbiprofen urea derivatives were synthesized bearing the thiadiazole ring. Their inhibition effects on tyrosinase were determined. 3c was found to be the strongest inhibitor with the IC50 value of 68.0 mu M against tyrosinase. The enzyme inhibition types of the synthesized compounds were determined by examining the kinetic parameters. The inhibition type of 3c was determined as uncompetitive and the K-i value was calculated as 36.3 mu M. Moreover, their cytotoxic effects on hepatocellular carcinoma (HepG2), colorectal carcinoma (HT-29), and melanoma (B16F10) cell lines were evaluated. According to the cytotoxicity results, 3l (IC50 = 14.11 mu M) showed the highest cytotoxicity on the HT-29 cells, while 3o (IC50 = 4.22 mu M) exhibited the strongest cytotoxic effect on HepG2 cell lines. Also, 3j (IC50 = 7.55 mu M strongly affected B16F10. The effects of synthesized compounds on the healthy cell line were evaluated on the CCD-986Sk cell line. Molecular modelling studies have indicated the potential binding interactions of the uncompetitive inhibitor 3c with the enzyme-substrate complex.
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    Synthesis of naproxen thiadiazole urea hybrids and determination of their anti-melanoma, anti-migration, tyrosinase inhibitory activity, and molecular docking studies
    (Elsevier, 2024) Kurt, Belma Zengin; Altundag, Ozlem; Gokce, Mustafa; Cakmak, Ummuhan; Tuncay, Fulya Oz; Kolcuoglu, Yakup; Akyildiz, Aysenur Gunaydin
    Novel sixteen naproxen urea compounds were synthesized bearing the thiadiazole ring. Their inhibitory activities against tyrosinase were investigated. 3o was discovered to be the most potent inhibitor of tyrosinase, with an IC50 value of 35.0 mu M. The kinetic parameters were used to determine the type of enzyme inhibition. The results showed that 3o was an uncompetitive inhibitor with the Ki value of 62.2 mu M. Additionally, the cytotoxic effects of the synthesized compounds on melanoma (B16F10), mouse embryonic (3T3) and the healthy 3T3 cell lines were also investigated. According to the cytotoxicity results, 3e (IC50= 2.17 mu M) showed the highest cytotoxicity on the B16F10 cells. Furthermore, the effects of selected compounds on the migration rate of melanoma cells were investigated. In addition, molecular modeling studies were also performed and the results showed the possible interactions between the uncompetitive inhibitor 3o with the Tyrosinase-L-Tyrosine enzyme substrate complex.