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SÜZGÜN, PELİN

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2013 - 201912020 - 20211
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Subject: ANTITUMOR-ACTIVITY ×

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    Recent Progress on Apoptotic Activity of Triazoles
    (BENTHAM SCIENCE PUBL LTD, 2021) SÜZGÜN, PELİN; Cikla-Suzgun, P.; Kucukguzel, S. G.
    Apoptosis is often called programmed cell death and is defined as a self-directed cell destruction process. It is different from necrosis due to the activation of caspases during this process. Apoptosis is directly related to cancer progression and plays a vital role in carcinogenesis; all cytotoxic drugs and radiation therapy programs initiate apoptosis in tumor cells. Today, studies show that heterocyclic compounds that contain triazole functionality have anticancer activities; triazoles are 5 membered rings, which contain two carbon and three nitrogen atoms. Therefore, many researchers have synthesized these small active compounds as target structures and evaluated their apoptotic activities. The present review describes recent medicinal aspects of triazoles as anticancer agents that have been reported during the past few years. We hope that the bioactivity of triazole derivatives will be beneficial for the rational design of a new generation of small molecule drugs.
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    Synthesis and characterization of flurbiprofen hydrazide derivatives as potential anti-HCV, anticancer and antimicrobial agents
    (SPRINGER BIRKHAUSER, 2013) TATAR, ESRA; Cikla, Pelin; Tatar, Esra; Kucukguzel, Ilkay; Sahin, Fikrettin; Yurdakul, Dilsad; Basu, Amartya; Krishnan, Ramalingam; Nichols, Daniel Brian; Kaushik-Basu, Neerja; Kucukguzel, S. Guniz
    A novel series of new flurbiprofen hydrazide derivatives 2-(2-fluorobiphenyl-4-yl)-N'-[(substituted phenyl/5-nitro-2-furyl)methylene]propanehydrazide (3a-k), 2-(2-fluorobiphenyl-4-yl)-N-(2-substituted-4-oxo-1,3-thiazolidine-3-yl)propanamide (4a-b, 4d-k), 2-[2-(2-fluorobiphenyl-4-yl) propanoyl]-N-substituted hydrazinecarbothioamide (5a-h) and 2-(2-fluorobiphenyl-4-yl)-N'-[(3-methyl-4-oxo-1,3-thiazolidin-2-ylidene]propanehydrazide (6a-b, 6e and 6g) has been synthesized in this study. All synthesized compounds were screened for antimicrobial activity against various bacterial and fungal strains. Additionally, compounds were evaluated for the ability to inhibit Hepatitis C virus NS5B polymerase. The most active 4-thiazolidinone compound was 4k (SGK119) with 67.0 % and thiosemicarbazide compound was 5d (SGK123) with 69.50 % inhibition at 200 mu M against hepatitis C virus NS5B RNA polymerase. Anticancer activity of the selected compounds (3i, 3j, 3h, 4d, 4i and 6b) was determined at a single dose towards the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI). 2-(2-Fluoro-4-biphenylyl)-N-[2-[4-(trifluoromethyl)phenyl]-4-oxo-1,3-thiazolidine-3-yl]propanamide 4d, containing thiazolidinone ring, demonstrated the most marked effect with 20.80 % growth percent on leukaemia cancer cell line SR at 10(-5) M. The results demonstrated that none of the compounds tested have anticandidal and antifungal activities, but two of them (4a and 4i) showed antibacterial inhibition against Micrococcus luteus, and Staphylococcus cohnii and Staphylococcus aureus, respectively.