Person: TOK, FATİH
Loading...
Email Address
Birth Date
Research Projects
Organizational Units
Job Title
Last Name
TOK
First Name
FATİH
Name
19 results
Search Results
Now showing 1 - 10 of 19
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 Metadata only Synthesis, anticancer evaluation and in silico ADMET studies on urea/thiourea derivatives from gabapentin(TAYLOR & FRANCIS LTD, 2020) KAYMAKÇIOĞLU, BEDİA; Turk, Sevda; Tok, Fatih; Erdogan, Omer; Cevik, Ozge; Tok, Tugba Taskin; Kocyigit-Kaymakcioglu, Bedia; Karakus, Sevgi2-(1-((3-Substitutedureido/thioureido)methyl)cyclohexyl)acetic acid derivatives (1-9) were synthesized from gabapentin. All the synthesized compounds were characterized by using IR, H-1-NMR, C-13-NMR spectroscopy, mass spectrometry and elemental analysis. Urea and thiourea derivatives were investigated for their potential in vitro anticancer activities on PC3 and MCF7 cancer cell lines using MTT assay. Cell apoptosis was detected by with Annexin V Assay. Our results showed that compound 8 {2-(1-((3-(2,6-dichlorophenyl)ureido)methyl)cyclohexyl)acetic acid} significantly inhibited the proliferation and growing of PC3 and MCF7 cells. Both cell types showed dysfunction of cellular morphology which induced apoptosis 10 mu M concentration of compound 8 treated cells. Our results indicate that compound 8 might have significance as an anti-tumor agent against human prostate and breast cancer. The theoretical structure and activity estimation via in silico ADMET was also examined.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 Metadata only Synthesis, biological evaluation and in silico studies of new pyrazoline derivatives bearing benzo[d]thiazol-2(3H)-one moiety as potential urease inhibitors(2022) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Baltaş, Nimet; Tatar, Gizem; Koçyiğit-Kaymakçıoğlu, BediaPublication Metadata only Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2021) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Ugras, Zefine; Saglik, Begum Nurpelin; Ozkay, Yusuf; Kaplancikli, Zafer Asim; Kocyigit-Kaymakcioglu, BediaThirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. IR, 1H-NMR, 13C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms. None of the compounds showed the potent MAO-A inhibitory activity, while the MAO-B inhibition was significantly found in the range of 62 to 98%. Among them, the compounds H8, H9 and H12 bearing chloro substituent at the fourth position of phenylurea were found to show potent monoamine oxidase B inhibitory activity with IC50 values 0.039-0.066 mu M. To define and evaluate the interaction mechanism between compound H8 and monoamine oxidase B, molecular docking studies have been made.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 Metadata only Design, synthesis and biological evaluation of some new 2-Pyrazoline derivatives as potential anticancer agents(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2020) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Abas, Burcin Irem; Cevik, Ozge; Kocyigit-Kaymakcioglu, BediaA new series of N-(4-(1-Phenyl-5-aryl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-4-substitutedbenzamide derivatives were designed and synthesized from new chalcone derivatives. All newly synthesized compounds were determined by using IR, H-1-NMR, C-13-NMR spectroscopic methods, elemental analysis and evaluated for their in vitro antiproliferative activities on HeLa, MCF-7, MKN-45 cancer cell lines and NIH-3T3 cell line using MTT assay. Expression of Bax and Bcl-2 proteins was detected by Western-blot analysis and caspase-3 enzyme activity was measured. Notably, compounds 1f and 2f showed a significant cytotoxic effect in all three cancer cells and did not display cytotoxicity on NIH-3T3 normal cells. (IC50 = 26.66 +/- 2.73 mu M on HeLa, IC50 = 9.41 +/- 2.19 mu M on MCF-7, IC50 = 5.17 +/- 3.54 mu M on MKN-45 for 1f. IC50 = 17.96 +/- 3.34 mu M on HeLa, IC50 = 0.69 +/- 0.13 mu M on MCF-7, IC50 = 0.88 +/- 0.16 mu M on MKN-45 for 2f.) Moreover, 1f and 2f upregulated protein expression level of Bax and downregulated protein expression level of Bcl-2 in cells. Similarly, caspase-3 activity was increased in cells via 1f and 2f. It can be concluded that 1f and 2f activated apoptosis by inducing mitochondrial apoptotic proteins in HeLa, MCF-7, MKN-45. This could be potentially new anti-cancer derivatives and used to contribute to new therapeutic development.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.