Person: TOK, FATİH
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TOK
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FATİH
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Publication Open Access Synthesis and anticancer activity of new carbohydrazide derivatives bearing furan moiety(MARMARA UNIV, 2022) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kaya Tilki, Elif; Dikmen, Miris; Kocyigit-Kaymakcioglu, BediaPublication Open Access Synthesis of some novel 1,3,4-oxadiazole derivatives and evaluation of their antimicrobial activity(2022-01-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., Kaya M., KARACA GENÇER H., KAYMAKÇIOĞLU B.Treatment for microbial infections still remains an important health problem for researchers around the world. Despite a broad range of antimicrobial drugs today, there are certain obstacles associated with the use of antimicrobial agents such as drug resistance and toxicity. Thus, medicinal chemists concentrate on designing novel antimicrobial drugs. In the search for new antimicrobial agents; 1,3,4-oxadiazole compounds have come forward due to their hydrolytic stability, good chemical and thermal stability. In the scope of this work, 2-(6-chloropyridin-3-yl)-5-(substitutedphenyl)-1,3,4-oxadiazole (4a-4i) were synthesizedusing 6-chloro-N\"-(substitutedbenzoyl)nicotinohydrazide (3a-3i). These compounds were screened for their antimicrobial activities against as gram-positive bacteria S. aureus, E. faecalis, as gram-negative bacteria E. coli, P. aeruginosa, as yeast C. parapsilosis, C. albicans, C. glabrata. Among the 1,3,4-oxadiazole compounds, 4h against E. faecalis and 4b, 4f and 4g against E. coli have been found to exhibit as much as potency chloramphenicol with MIC50 values of 62.50 mu g/mL.Publication Open Access Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives(SLOVENSKO KEMIJSKO DRUSTVO, 2020-12-15) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaymakcioglu, Bedia1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, H-1 NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the alpha-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 mu M) and their IC50 values were in the range of 0.68 and 4.45 mu M. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski's and Veber's rules.Publication Open Access Synthesis of novel pyrazoline derivatives and evaluation of their antimicrobial activity(2022-01-01) TOK, FATİH; GÜRBÜZ, BURÇAK; KAYMAKÇIOĞLU, BEDİA; TOK F., Doğan M. O. , GÜRBÜZ B., Koçyiğit-Kaymakçioğlu B.© 2022 Marmara University Press.In this study, new nine pyrazoline derivatives were synthesized from chalcone derivatives. The antimicrobial activity of nine pyrazoline derivatives to four standard bacterial strains (Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis) and four standard yeast strains (Candida albicans, Candida glabrata, Candida parapsilosis, Candida tropicalis) was investigated by the microdilution method for in accordance with the Clinical and Laboratory Standards Institute (CLSI) standard, and the Minimal Inhibitory Concentration (MIC) values of these derivatives were determined. Among these derivatives; compounds 7 and 8 against bacterial strains and compounds 2 and 3 against yeast strains exhibited good antimicrobial activity.Publication Open Access Design, synthesis, in silico ADMET studies and anticancer activity of some new pyrazoline and benzodioxole derivatives(2022-01-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., ERDOĞAN Ö., ÇEVİK Ö., KAYMAKÇIOĞLU B.A new series of 2-pyrazoline derivatives starting from substituted benzodioxole chalcones were designed and synthesized. IR and 1H NMR spectral data and elemental analysis were used to characterize the structures of the synthesized compounds. The cytotoxic activities on HeLa, MCF-7 cancer cell lines and NIH-3T3 for these compounds were tested by using MTT assay. Among the synthesized compounds 2d, 2j, 3j and 3n against MCF-7 cells, and 3c against HeLa exhibited significant cytotoxic activity with IC50 between 10.08 and 27.63 mu M. Compound 3f showed the most potent anticancer activity against both cancer cells with good selectivity (IC50 = 11.53 mu M on HeLa with SI = 81.75 and IC50 = 11.37 mu M on MCF-7 with SI = 82.90). Furthermore, in silico ADMET analyses were performed and the drug-likeness properties of the compounds were investigated.Publication Open Access N-Substituted Arylidene-3-(Methylsulfonyl)-2-Oxoimidazolidine-1-Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study(2022-08-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., SAĞLIK B. N., ÖZKAY Y., KAPLANCIKLI Z. A., KAYMAKÇIOĞLU B.The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer\"s disease (AD), have been designed and synthesized. The acetylcholinesterase (AChE) enzyme inhibitory activity of these compounds was investigated. The structures of the compounds were determined by IR, H-1 and C-13-NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes and beta-amyloid plaque inhibition test of the compounds were performed. Based on the experimental results, compound 3j bearing dimethoxy substituent on the aromatic ring like donepezil exhibited the most AChE inhibitory activity with the IC50 values of 0.023 +/- 0.001 mu M. Owing to obtained biological activity and molecular docking study results, it is thought that the most active compound 3j may play a role in both symptomatic and palliative treatment of AD.Publication Open Access Synthesis of novel thiosemicarbazone derivatives as antidiabetic agent with enzyme kinetic studies and antioxidant activity(2022-01-01) KAYMAKÇIOĞLU, BEDİA; TOK, FATİH; TOK F., KÜÇÜKAL B., BALTAŞ N., Yilmaz G. T., KAYMAKÇIOĞLU B.Novel thiosemicarbazone derivatives were synthesized via condensation reactions between the corresponding thiosemicarbazides and 4-(methylsulfonyl)acetophenone. The chemical structures of all compounds were elucidated by infrared (IR), H-1-NMR and C-13-NMR spectroscopy and mass spectrometry. Antioxidant studies of all compounds were performed by using CUPRAC, FRAP, DPPH methods. 2-{1-[4-(Methylsulfonyl)phenyl]ethylidene}-N-phenylhydrazinecarbothioamide (1) possessed good antioxidant activity with an SC50 value of 15.70 mu M which also is higher than standard drug, ascorbic acid. All compounds were evaluated for their antidiabetic properties as alpha-glycosidase and alpha-amylase inhibitors. Compound 1 was found to be the most active compound against alpha-glucosidase and alpha-amylase with IC50 values of 1.58 mu M and 3.24 mu M, respectively. The enzyme kinetic studies demonstrated that compound 1 has a competitive mode of binding. Furthermore, molecular docking studies have elucidated the binding mechanism at the molecular level by examining the molecular interactions between compound 1 and these enzymes.Publication Open Access Synthesis of phthalimide derivatives and their insecticidal activity against caribbean fruit fly, anastrepha suspensa (Loew)(2023-02-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., Yang X., Tabanca N., Koçyiğit-Kaymakçıoğlu B.In this study, thirteen phthalimide derivatives were designed and synthesized. All synthesized compounds were evaluated to determine their potential for inhibitory activities against females of the Caribbean fruit fly, Anastrepha suspensa (Loew) (Diptera: Tephritidae). These efforts led to the discovery of three compounds 4a, 4c, and 4d with potent insecticidal activity (LD50 range from 0.70 to 1.91 μg/fly). Among these compounds, 4a exhibited the highest inhibitory potency with 0.70 μg/fly. In addition, in silico models indicated that compound 4a is less toxic than phthalimide and other precursors. Therefore, our results suggest that 4a has strong potential as a candidate component for developing a novel environmentally friendly insecticide for control of pest fruit flies.Publication Open Access Design, synthesis, biological activity evaluation and in silico studies of new nicotinohydrazide derivatives as multi-targeted inhibitors for Alzheimer's disease(2022-10-01) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; TOK F., SAĞLIK B. N., ÖZKAY Y., KAPLANCIKLI Z. A., KAYMAKÇIOĞLU B.A new series of 6-chloro-N\"-(substituted benzylidene)nicotinohydrazide were synthesized via condensation reactions between the corresponding hydrazides and aldehydes . All compounds were tested for their AChE and BuChE inhibitory activity. Compounds P5, P7, P9, P10 and P12 exhibited significant AChE inhibition potencies. Among them, compound P5 having para nitro substituent was found to be the most effective derivative against AChE with an IC50 value of 0.027 +/- 0.001 mu M. After that, the BACE-1 and beta-amyloid plaque inhibitory potencies of selected compounds P5, P7, P9, P10 and P12 were evaluated. Among them, compound P5 displayed the highest inhibition rate against the BACE-1 enzyme and beta-amyloid plaque. Molecular docking studies were carried out using both AChE and BACE-1 crystals to determine the compound\"s interactions with the enzyme\"s active sites. Furthermore, we evaluated the ADMET properties of compounds and their blood-brain barrier (BBB) permeation was also found to be high. (C) 2022 Elsevier B.V. All rights reserved.Publication Open Access Antiproliferative activity of some tautomeric hydrazones derived from chalcones(MARMARA UNIV, FAC PHARMACY, 2016-02-02) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Beyhan, Nagihan; Erzurumlu, Yalcin; Ilhan, Recep; Ballar, Petek; Kocyigit-Kaymakcioglu, BediaA new series of hydrazones synthesized from chalcones. Synthesized compounds have been characterized by IR, H-1-NMR and elemental analysis. Antiproliferative activity of compounds was investigated on Hela, A549, MCF7, HCC1937, MRC5 cells. All compounds exhibited cytotoxicity. Especially compounds 1b, 1c, 1f and 1i having 4-metylsulfonyl phenyl showed higher cytotoxicity against all of the cell lines compared to reference drug doxorubicin with low value of IC50=5,56-21,93 mu M. The most active compounds 1b, 1c, 1f and 1i were analyzed for their effect on autophagic processes. HCC1937 cells were treated with these compounds at IC50 concentration for 24 hours. An immunoblotting assay was performed to analysis autophagy markers and total polyubiquitinated protein levels. Compounds 1b, 1c, 1f and 1i significantly increased the conversion of LC3-I to LC3-II at IC50 concentration. None of the tested compounds changed the level of total polyubiquitinated proteins.