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This site is Bezmialem Vakif University Academic Open Access System. The system was established in June 2019 in order to store the academic outcomes of Bezmialem Vakif University in digital standards and to provide them with open access. OpenAccess includes academic outputs such as articles, presentations, dissertations, books, book chapters and reports produced by Bezmialem Vakif University.

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Synthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studies
(2023-01-01) ZENGİN KURT B.; Altundağ Ö.; Tokgöz M. N.; ÖZTÜRK CİVELEK D.; Tuncay F. O.; Cakmak U.; KOLCUOĞLU Y.; Akdemir A.; Sönmez F.; ZENGİN KURT, BELMA; ÖZTÜRK CİVELEK, DİLEK
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 μM 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 Ki value was calculated as 36.3 μM. 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 μM) showed the highest cytotoxicity on the HT-29 cells, while 3o (IC50 = 4.22 μM) exhibited the strongest cytotoxic effect on HepG2 cell lines. Also, 3j (IC50 = 7.55 μM 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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