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SÜZGÜN, PELİN

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Author: BİNGÖL ÖZAKPINAR, ÖZLEM × Subject: 4-Thiazolidinone ×

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    Synthesis, Cytotoxicity, and Pro-Apoptosis Activity of Etodolac Hydrazide Derivatives as Anticancer Agents
    (WILEY-V C H VERLAG GMBH, 2013) ŞENER, AZİZE; Cikla, Pelin; Ozsavci, Derya; Bingol-Ozakpinar, Ozlem; Sener, Azize; Cevik, Ozge; Ozbas-Turan, Suna; Akbuga, Julide; Sahin, Fikrettin; Kucukguzel, S. Guniz
    Etodolac hydrazide and a novel series of etodolac hydrazide-hydrazones 315 and etodolac 4-thiazolidinones 1626 were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, 1H NMR, 13C NMR, HREI-MS) methods. Some selected compounds were determined at one dose toward the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI, Bethesda, USA). 2-(1,8-Diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(4-chlorophenyl)methylene]hydrazide 9 demonstrated the most marked effect on the prostate cancer cell line PC-3, with 58.24% growth inhibition at 105M (10 mu M). Using the MTT colorimetric method, compound 9 was evaluated in vitro against the prostate cell line PC-3 and the rat fibroblast cell line L-929, for cell viability and growth inhibition at different doses. Compound 9 exhibited anticancer activity with an IC50 value of 54 mu M (22.842 mu g/mL) against the PC-3 cells and did not display any cytotoxicity toward the L-929 rat fibroblasts, compared to etodolac. In addition, this compound was evaluated for caspase-3 and Bcl-2 activation in the apoptosis pathway, which plays a key role in the treatment of cancer.