Person: ŞENKARDEŞ, SEVİL
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ŞENKARDEŞ
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SEVİL
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Publication Open Access Synthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agents(MDPI, 2013-03-21) ŞENER, AZİZE; Kucukguzel, S. Guniz; Coskun, Inci; Aydin, Sevil; Aktay, Goknur; Gursoy, Sule; Cevik, Ozge; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Sener, Azize; Kaushik-Basu, Neerja; Basu, Amartya; Talele, Tanaji T.A series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides 2a-e were synthesized by the addition of ethyl alpha-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)- 1H-pyrazol-1-yl] benzene sulfonamides 1a-e, which were synthesized by the reaction of alkyl/aryl isothiocyanates with celecoxib. The structures of the isolated products were determined by spectral methods and their anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV NS5B RNA-dependent RNA polymerase (RdRp) activities evaluated. The compounds were also tested for gastric toxicity and selected compound 1a was screened for its anticancer activity against 60 human tumor cell lines. These investigations revealed that compound 1a exhibited anti-inflammatory and analgesic activities and further did not cause tissue damage in liver, kidney, colon and brain compared to untreated controls or celecoxib. Compounds 1c and 1d displayed modest inhibition of HCV NS5B RdRp activity. In conclusion, N-(ethylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide (1a) may have the potential to be developed into a therapeutic agent.Publication Open Access A Novel Anti-Hepatitis C Virus and Antiproliferative Agent Alters Metabolic Networks in HepG2 and Hep3B Cells(MDPI, 2017-06-02) ŞENKARDEŞ, SEVİL; Keogh, Adrian; Senkardes, Sevil; Idle, Jeffrey R.; Kucukguzel, S. Guniz; Beyoglu, DirenA series of novel diflunisal hydrazide-hydrazones has been reported together with their anti-hepatitis C virus and antiproliferative activities in a number of human hepatoma cell lines. However, the mechanisms underlying the efficacy of these agents remain unclear. It was chosen to investigate the lead diflunisal hydrazide-hydrazone, 2',4'-difluoro-4-hydroxy-N'-[(pyridin-2-yl) methylidene] biphenyl-3-carbohydrazide (compound 3b), in two cultured human hepatoma cell lines-HepG2 and Hep3B-using a metabolomic protocol aimed at uncovering any effects of this agent on cellular metabolism. One sub-therapeutic concentration (2.5 mu M) and one close to the IC50 for antimitotic effect (10 mu M), after 72 h in cell culture, were chosen for both compound 3b and its inactive parent compound diflusinal as a control. A GCMS-based metabolomic investigation was performed on cell lysates after culture for 24 h. The intracellular levels of a total of 42 metabolites were found to be statistically significantly altered in either HepG2 or Hep3B cells, only eight of which were affected in both cell lines. It was concluded that compound 3b affected the following pathways-purine and pyrimidine catabolism, the glutathione cycle, and energy metabolism through glycolysis and the pentose phosphate pathway. Although the metabolomic findings occurred after 24 h in culture, significant cytotoxicity of compound 3b to both HepG2 and Hep3B cells at 10 mu M were reported not to occur until 72 h in culture. These observations show that metabolomics can provide mechanistic insights into the efficacy of novel drug candidates prior to the appearance of their pharmacological effect.Publication Metadata only Synthesis, molecular docking and evaluation of novel sulfonyl hydrazones as anticancer agents and COX-2 inhibitors(SPRINGER, 2020) KÜÇÜKGÜZEL, İLKAY; Senkardes, Sevil; Han, M. Ihsan; Kulabas, Necla; Abbak, Muruvvet; Cevik, Ozge; Kucukguzel, Ilkay; Kucukguzel, S. GunizIn trying to develop new anticancer agents, a series of sulfonylhydrazones were synthesized. All synthesized compounds were checked for identity and purity using elemental analysis, TLC and HPLC and were characterized by their melting points, FT-IR and NMR spectral data. All synthesized compounds were evaluated for their cytotoxic activity against prostate cancer (PC3), breast cancer (MCF-7) and L929 mouse fibroblast cell lines. Among them,N '-[(2-chloro-3-methoxyphenyl)methylidene]-4-methylbenzenesulfonohydrazide(3k)showed the most potent anticancer activity against both cancer cells with good selectivity (IC50 = 1.38 mu M on PC3 with SI = 432.30 and IC50 = 46.09 mu M on MCF-7 with SI = 12.94). Further investigation confirmed that3kdisplayed morphological alterations in PC3 and MCF-7 cells and promoted apoptosis through down-regulation of the Bcl-2 and upregulation of Bax expression. Additionally, compound3kwas identified as the most potent COX-2 inhibitor (91% inhibition) beside lower COX-1 inhibition. Molecular docking of the tested compounds represented important binding modes which may be responsible for their anticancer activity via inhibition of the COX-2 enzyme. Overall, the lead compound3kdeserves further development as a potential anticancer agent. [GRAPHICS] .Publication Metadata only Quorum Sensing Inhibitor Activities of Celecoxib Derivatives in Pseudomonas aeruginosa(BENTHAM SCIENCE PUBL LTD, 2017) TINAZ, GÜLGÜN; Ulusoy, Seyhan; Senkardes, Sevil; Coskun, Inci; Bosgelmez-Tinaz, Gulgun; Soulere, Laurent; Queneau, Yves; Kucukguzel, S. GunizBackground: A series of novel N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)3-( trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamides [SGK 318, 319, 320, 324, 327] and N-(3-substitutedaryl/ alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides[SGK 328, 329, 330, 334, 337] were synthesized and tested for their quorum sensing inhibitor (QSI) capacity using quorum sensing inhibitor selector 1 (QSIS1) bioassay. Findings: QSIS assay revealed that SGK 324, SGK 327 and SGK 330 have the potentials to interfere with QS system in QS inhibitor selector1 (QSIS1) reporter strain. Moreover, these compounds were found to significantly affect QS regulated elastase and biofilm productions in Pseudomonas aeruginosa PA01 strain without affecting its growth. Molecular modeling experiments suggested that SGK 330 fits within the binding site of LasR protein of P. aeruginosa. SGK 324 and 327 also bind LasR provided that they adopt a s-trans/s-cis conformation with respect to the thiourea function. Results and Conclusion: Results of this study indicated that these compounds could be developed as new QS inhibitors without killing the bacteria but as antivirulence compounds to restrict virulence of clinically important human pathogens.Publication Metadata only Synthesis of Diflunisal Thiazolidinones as Anticancer Agents(BENTHAM SCIENCE PUBL LTD, 2016) ŞENER, AZİZE; Senkardes, Sevil; Ozakpinar, Ozlem B.; Ozsavci, Derya; Sener, Azize; Cevik, Ozge; Kucukguzel, S. GunizA series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2',4'-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl-3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 mu M. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH-3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC50 value of 5.2 mu M against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.Publication Metadata only Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from N-(arylsulfonyl)methionine(SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2016) TATAR, ESRA; Tatar, Esra; Senkardes, Sevil; Sellitepe, Hasan Erdinc; Kucukguzel, Sukriye Guniz; Karaoglu, Sengul Alpay; Bozdeveci, Arif; De Clercq, Erik; Pannecouque, Christophe; Ben Hadda, Taibi; Kucukguzel, IlkayA series of 38 new acylhydrazones [3-40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity with the further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess stronger activity against gram (+) bacteria. Compound 23 was found active against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 mu g/mL. The MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 mu g/mL. A computational study for prediction of ADME and drug-like properties (solubility, drug-likeness, and drug score) as well as potential toxicity profiles of compounds 2-40 was performed using the Molinspiration online property calculation toolkit and Osiris Property Explorer. As most of our compounds meet Lipinski's rule of five, they promise good solubility and permeability. According to Osiris calculations, the majority of our compounds are supposed to be nonmutagenic and nonirritating.Publication Metadata only Synthesis of 1-aroyl-3,5-dimethyl-1H-pyrazoles as anti-HCV and anticancer agents(2014) ORUN, OYA; Aydin S., Kaushik-Basu N., Özbaş-Turan S., Akbuǧa J., Tiber P.M., Orun O., Gurukumar K.R., Basu A., Küçükgüzel Ş.G.1-Aroyl-3,5-dimethyl-1H-pyrazole derivatives (7-12) were synthesized from some hydrazides (1-6) with acetylacetone (2,4-pentanedione) by microwave irradiation. Their structures were elucidated by FT-IR and 1H-NMR spectral data and elemental analysis. Compound activities were evaluated against HCV NS5B and in cell based HCV reporters. Compound 8 was the most promising of this series in inhibiting intracellular NS5B activity and HCV RNA replication in reporter cells. The selected compounds 9, 10 and 12 by National Institue of Health were screened for their anticancer activity against 60 human tumor cell lines. Compound 9 (3-[(3,5-dimethyl-1H-pyrazol-1-yl)carbonyl]-2′,4′- difluorobiphenyl-4-ol) possessed significant activity against human immortalized myelogenous leukemia (K-562) exhibiting cell growth promotion 30.05%, with inhibition of 69.95% at 10-5M concentration. Compounds 3 and 9 were evaluated for cell viability and growth inhibition by K-562 cells of MTT assay, at different doses (10-6- 10-2M). Further, compound 9 exhibited anticancer activity against K-562 cells with IC50 value of 4 μM . Apoptosis levels of compound 9 were determined for three different concentrations (10-6, 10-5 and 10-3M) at two time points (24 and 48 h). Compound 9 induced apoptosis of K-562 cells, thus suggesting that compound 9 might be a potential chemopreventive agent for chronic myelogenous leukemia. © 2014 Bentham Science Publishers.Publication Open Access Synthesis and anticancer activity of novel hydrazone linkage-based aryl sulfonate derivatives as apoptosis inducers(SPRINGER BIRKHAUSER, 2022-02) BİNGÖL ÖZAKPINAR, ÖZLEM; Senkardes, Sevil; Han, M. Ihsan; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. GunizIn the present study, the various 28 hybrid molecules containing hydrazone and sulfonate moieties were synthesized and characterized by FTIR, H-1-NMR, C-13-NMR spectroscopy and LC-MS spectrometry, besides elemental analysis. The compounds were evaluated for their antiproliferative effects against six cancer cell lines, namely A549 (non-small cell lung cancer), MCF-7 (breast cancer), HT-29 (colorectal adenocarcinoma cancer), PC-3 (androgen-independent prostate adenocarcinoma), Hep3B (hepatocellular carcinoma cancer), and HeLa (epitheloid cervix carcinoma cancer). Among all the target compounds, compounds 4g and 4h exhibited more promising effects on MCF-7 cell lines (IC50 = 17.8 mu M and 21.2 mu M, respectively) with high selectivity. Further mechanistic studies proposed that compounds 4g and 4h induced apoptosis is mediated through the intrinsic apoptotic pathway with changes in mitochondrial membrane potential by finally activating caspase-9 and caspase-3. The results have been encouraging enough to merit further investigation. [GRAPHICS] .Publication Open Access Synthesis, molecular docking studies and ADME prediction of some new albendazole derivatives as α-Glucosidase inhibitors(2022-08-01) ŞENKARDEŞ, SEVİL; Şenkardeş S.Publication Metadata only Synthesis, characterization and in silico adme screening of somenew 1,3-thiazole derivatives(2021-04-17) ŞENKARDEŞ, SEVİL; ŞENKARDEŞ S., EKREK S.
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