Person: SÜZGÜN, PELİN
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SÜZGÜN
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PELİN
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Publication Metadata only Recent advances bioactive 1,2,4-triazole-3-thiones(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2015) SÜZGÜN, PELİN; Kucukguzel, S. Guniz; Cikla-Suzgun, PelinTriazoles are heterocyclic compounds which have a five-membered ring of two carbon atoms and three nitrogen atoms. These structures have been interest in the development of novel compounds with anticonvulsant, antidepressant, antioxidant, anti-inflammatory, analgesic, antinociceptive, antibacterial, antimycobacterial, antifungal, antiviral, anticancer, anti-parasitic, anti-urease and other activities. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. This review contains various pharmacological activities of 1,2,4-triazole-3-thiones in one place and it is also the milestone for the new research towards this moiety. (C) 2014 Elsevier Masson SAS. All rights reserved.Publication Open Access Etodolac Thiosemicarbazides:A novel class of hepatitis C virus NS5B polymerase inhibitors(2013-01-01) SÜZGÜN, PELİNPublication Open Access Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles(TAYLOR & FRANCIS LTD, 2015-09-03) SÜZGÜN, PELİN; Cikla-Suzgun, Pelin; Kaushik-Basu, Neerja; Basu, Amartya; Arora, Payal; Talele, Tanaji T.; Durmaz, Irem; Cetin-Atalay, Rengul; Kucukguzel, S. GunizArachidonic acid is an unsaturated fatty acid liberated from phospholipids of cell membranes. NSAIDs are known as targets of cyclooxygenase enzyme (COX-1, COX-2 and COX-3) in arachidonic acid metabolism. This mechanism of COX-2 in carcinogenesis causes cancer. In addition, COX-2 plays a role in the early stages of hepatocarcinogenesis. Hepatitis C virus (HCV) infection is cause of liver cirrhosis and hepatocellular carcinoma (HCC). The aim of our study was to improve effective agents against HCV. A novel series of new etodolac 1,2,4-triazoles derivatives (4a-h) have been synthesized and investigated for their activity against HCV NS5B polymerase. Compound 4a was found to be the most active with IC50 value of 14.8 mu M. In accordance with these results, compound 4a was screened for anti-cancer activity on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS). Compound 4a showed anti-cancer activity against Huh7 human hepatoma cell line with IC50 value of 4.29 mu M. Therefore, compound 4a could be considered as a new anti-cancer and anti-HCV lead compound.Publication Metadata only Synthesis and evaluation of antiviral, antitubercular and anticancer activities of some novel thioureas derived from 4-aminobenzohydrazide hydrazones [4-Aminobenzohidrazit hidrazonlarından türetilmiş bazı yeni tiyoürelerin sentezi, antiviral, antitüberküler ve antikanser etkilerinin deǧerlendirilmesi](Marmara University, 2010) KÜÇÜKGÜZEL, İLKAY; Çikla P., Güniz Küçükgüzel Ş., Küçükgüzel I., Rollas S., De Clercq E., Pannecouque C., Andrei G., Snoeck R., Şahin F., Bayrak Ö.F.A series of novel 1-[4-[[2-[(4-substituted phenyl)methylene]hydrazino]carbonyl]p henyl]-3-substituted thiourea derivatives have been synthesized by the addition of substituted aryl isothiocyanates to 4-amino-N'-[(4-substituted phenyl) methylene] benzohydrazide, which was prepared by condensation of 4-aminobenzoic acid hydrazide with 4-fluorobenzaldehyde or 4-(trifluoromethyl)benzaldeyde. All synthesized compounds were evaluated in vitro against HIV-1 (IIIB) and HIV-2 (ROD) strains in MT-4 cells, as well as other selected viruses such as HSV-1, HSV-2, Coxsackie virus B4, Sindbis virus, human cytomegalovirus, and varicella-zoster virus using HeLa, Vero, or HEL cell cultures. Antimycobacterial activity against Mycobacterium tuberculosis H37 Rv was also evaluated. The anticancer activity and cytotoxicity screening of the synthesized compounds were determined on A 549 and L 929 cell lines.Publication Metadata only Recent Advances in Apoptosis: The Role of Hydrazones(BENTHAM SCIENCE PUBL LTD, 2019) SÜZGÜN, PELİN; Cikla-Suzgun, Pelin; Kucukguzel, S. GunizThe process of programmed cell death in higher eukaryotes (apoptosis), is generally characterized by distinct morphological characteristics and energy-dependent biochemical mechanisms. Apoptosis is considered as a vital component of various processes including normal cell turnover, proper development and functioning of the immune system, hormone-dependent atrophy, embryonic development and chemical-induced cell death. Apoptosis seems to play an important key role in the progression of several human diseases like Alzheimer's disease, Parkinson's disease and many types of cancer. Promotion of apoptosis may be a good approach for the prevention of cancer cell proliferation. In early studies, antitumor compounds have been found to induce the apoptotic process in tumor cells. On the other hand, several hydrazones were reported to have lower toxicity than hydrazides due to the blockage of -NH2 group. Therefore, the design of hydrazones that activate and promote apoptosis is an attractive strategy for the discovery and development of potential anticancer agents. The aim of this review is to provide a general overview of current knowledge and the connection between apoptosis and hydrazone. It is also the guide for the apoptotic activities of new hydrazone derivatives.Publication Metadata only Synthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells(WILEY-V C H VERLAG GMBH, 2015) ÖZSAVCI, DERYA; Kucukguzel, S. Guniz; Koc, Derya; Cikla-Suzgun, Pelin; Ozsavci, Derya; Bingol-Ozakpinar, Ozlem; Mega-Tiber, Pinar; Orun, Oya; Erzincan, Pinar; Sag-Erdem, Safiye; Sahin, FikrettinTolmetin hydrazide and a novel series of tolmetin hydrazide-hydrazones 4a-l were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, H-1 NMR) methods. N-[(2,6-Dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) was evaluated in vitro using the MTT colorimetric method against the colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) to determine growth inhibition and cell viability at different doses. Compound 4g exhibited anti-cancer activity with an IC50 value of 76M against colon cancer line HT-29 (ATCC, HTB-38) and did not display cytotoxicity toward control NIH3T3 mouse embryonic fibroblast cells compared to tolmetin. In addition, this compound was evaluated for caspase-3, caspase-8, caspase-9, and annexin-V activation in the apoptotic pathway, which plays a key role in the treatment of cancer. We demonstrated that the anti-cancer activity of this compound was due to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway. In addition, in this study, we investigated the catalytical effect of COX on the HT-29 cancer line, the apoptotic mechanism, and the moleculer binding of tolmetin and compound 4g on the COX enzyme active site.Publication Open Access Effect of etodolac hydrazone, a new compound synthesised from etodolac, on spermatozoon quality, testicular lipid peroxidation, apoptosis and spermatozoon DNA integrity(WILEY, 2016-03) SÜZGÜN, PELİN; Sariozkan, S.; Turk, G.; Cikla-Suzgun, P.; Guvenc, M.; Yuce, A.; Yay, A. H.; Canturk, F.; Kucukguzel, S. G.The aim of this study was to investigate the effect of etodolac hydrazone (EH), a new compound synthesised from etodolac, on spermatozoon quality, testicular lipid peroxidation, apoptosis and spermatozoon DNA integrity in rats. Group 1 (n=8) received 1ml dimethyl sulfoxide (DMSO) daily (Control); group 2 (n=8) was treated with 5mgkg(-1)day(-1) EH, dissolved in 1ml DMSO (EH-5); and group 3 (n=8) was treated with 10 mg kg(-1)day(-1) EH, dissolved in 1ml DMSO (EH-10). All administrations were performed by gavage and maintained for 8weeks. Both doses of EH administration caused significant decreases in absolute and relative weights of testis, whole epididymis, right cauda epididymis, and spermatozoon motility, spermatozoon count in comparison with the control group. Only 10mgkg(-1)day(-1) EH administration caused significant decreases in absolute and relative weights of seminal vesicles and serum testosterone level, and significant increases in testicular lipid peroxidation level, and numbers of TUNEL+ apoptotic germ cells and spermatozoa with damaged DNA along with some histopathological damages when compared to the control group. However, body and ventral prostate weight, and testicular antioxidant markers (glutathione, glutathione-peroxidase and catalase), were unaffected significantly by both doses of EH administration. In conclusion, two different doses of EH, in particular its high dose, damage to testicular spermatogenic cells and spermatozoon DNA and, it decreases spermatozoon motility, count and testosterone level in healthy rats.Publication Metadata only 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. GunizEtodolac 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.Publication Metadata only 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.Publication Metadata only 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. GunizA 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.