Person: TOK, FATİH
Loading...
Email Address
Birth Date
Research Projects
Organizational Units
Job Title
Last Name
TOK
First Name
FATİH
Name
40 results
Search Results
Now showing 1 - 10 of 40
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 Metadata only Synthesis of new hydrazone derivatives bearing imidazolidine Moiety as monoamine Oxidase inhibitors(2021-12-02) TOK, FATİH; TOK F., SAĞLIK B. N.Publication 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 Metadata only Synthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaymakcioglu, Bedia; Saglik, Begum Nurpelin; Levent, Serkan; Ozkay, Yusuf; Kaplancikli, Zafer AsimIn the current work, Schiff base derivatives of antipyrine were synthesized. The chemical characterization of the compounds was confirmed using IR, H-1 NMR, C-13 NMR and mass spectroscopies. The inhibitory potency of synthesized compounds was investigated towards acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases A and B (MAO-A and MAO-B) enzymes. Some of the compounds displayed significant inhibitory activity against AChE and MAO-B enzymes, respectively. According to AChE enzyme inhibition assay, compounds 3e and 3g were found as the most potent derivatives with IC50 values of 0.285 mu M and 0.057 mu M, respectively. Also, compounds 3a (IC50 = 0.114 mu M), 3h (IC50 = 0.049 mu M), and 3i (IC50 = 0.054 mu M) were the most active derivatives against MAO-B enzyme activity. So as to understand inhibition type, enzyme kinetics studies were carried out. Furthermore, molecular docking studies were performed to define and evaluate the interaction mechanism between compounds 3g and 3h and related enzymes. ADME (Absorption, Distribution, Metabolism, and Excretion) and BBB (Blood, Brain, Barier) permeability predictions were applied to estimate pharmacokinetic profiles of synthesized compounds.Publication Metadata only Design, synthesis, biological evaluation and molecular docking of novel molecules to PARP-1 enzyme(SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2019) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Kocyigit-Kaumakcioglu, Bedia; Ilhan, Recep; Yilmaz, Sinem; Ballar-Kirmizibayrak, Petek; Taskim-Tok, TugbaPoly (ADP-ribose) polymerase (PARP) enzyme catalyzes the transfer of ADP-ribose into target proteins. Therefore, PARP is responsible for DNA repair, cell proliferation, and cell death. In this study, potential PARP enzyme inhibitors were designed and synthesized. The synthesized compounds were elucidated by Fourier-transform infrared spectroscopy, H-1 NMR, C-13 NMR, heteronuclear single-quantum correlation, and mass spectrometry, and their purity was checked via thin-layer chromatography, high-performance liquid chromatography, and elemental analysis. A total of 63 newly synthesized compounds were screened in terms of PARP inhibition by cellular PARylation assay in the HeLa cell line. It was found that 19 compounds significantly inhibited the H2O2-induced cellular PARylation. The chemosensitizer effect of these compounds in cancer cells treated with doxorubicin (doxo) was investigated. It was found that the combination of potent PARP inhibitors with doxo potentiated a cytotoxic effect, similar to that of olaparib. The results of the molecular docking and absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis revealed that compound 60 might be classified as a potential PARP inhibitor candidate. Taken together, all of the results suggested that carbohydrazide derivatives could be a promising lead for the treatment for cancer disorders.Publication Open Access Synthesis, characterization and biological evaluation of novel thiourea derivatives(2022-06-01) TOK, FATİH; TOK F., Cakir C., Cam D., Kirpat M. M., SICAK Y.Objective: A new series of 4-[3-(substitutedphenyl)thioureido]-N-(6-chloropyrazin-2-yl)benzenesulfonamide were synthesized from sulfaclozine. Methods: All compounds were characterized by IR, 1 H-NMR spectroscopic methods and elemental analysis. In addition to the antioxidant activity of the synthesis series, enzyme inhibition activities such as anticholinesterase, tyrosinase, α-amylase and α-glycosidase were determined for the first time in this study. Results: According to these biological activity test results, compound 2a in the DPPH, 2c in the ABTS˙+ assay exhibited more antioxidant activity than reference standard. All thiourea derivatives demonstrated good BChE inhibitory activity than galantamine. Among the compounds, 2e and 2f showed the best tyrosinase enzyme inhibition activity, while 2g had the best α-amylase and α-glucosidase enzyme inhibition activity. In addition, we evaluated the druglikeness properties of compounds and their oral bioavailability were also found to be high. Conclusion: Thiourea derivatives exhibited remarkable antioxidant activity and enzyme inhibition activity against tyrosinase, cholinesterase, α-amylase and α-glucosidasePublication Metadata only Synthesis and in silico ADME studies of new phthalimide derivatives(2022-09-25) TOK, FATİH; TOK F.Publication Metadata only Pirazolon halkası taşıyan bazı Schiff bazlarının biyolojik etkilerinin incelenmesi(2018-11-16) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; UĞRAŞ Z., TOK F., KAYMAKÇIOĞLU B.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.