Person: TOK, FATİH
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TOK
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FATİH
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Publication 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 Metadata only Synthesis and in silico ADME studies of new phthalimide derivatives(2022-09-25) TOK, FATİH; TOK F.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 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 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 Metadata only Synthesis and antimicrobial evaluation of new pyrazoline derivatives(2022-05-28) GÜRBÜZ, BURÇAK; TOK, FATİH; Tok F., Gürbüz B.Publication Metadata only Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2021) KAYMAKÇIOĞLU, BEDİA; Tok, Fatih; Saglik, Begum Nurpelin; Ozkay, Yusuf; Ilgin, Sinem; Kaplancikli, Zafer Asim; Kocyigit-Kaymakcioglu, BediaA novel series of hydrazone derivatives were designed and synthesized. Their structures were characterized by IR, 1H NMR, 13C NMR and HR-MS spectroscopic methods. The newly synthesized compounds were evaluated for their inhibitory activity against monoamine oxidase enzymes (MAO-A and MAO-B). Compounds 2a, 2k, 4a and 4i showed significant inhibitory activity against MAO-A, with IC50 value in the range of 0.084-0.207 mu M compared to reference drug moclobemide (IC50 value = 6.061 mu M). These compounds (2a, 2k, 4a and 4i) were exposed to cytotoxicity tests to establish their preliminary toxicological profiles and were found to be noncytotoxic. Moreover, the most effective compound 4i was evaluated using enzyme kinetics and docking studies to elucidate the plausible mechanisms of inhibition of MAO-A. According to enzyme kinetic studies, compound 4i was a reversible and competitive inhibitor with similar inhibition features as the substrates. Also, it was seen that this compound was settled down very properly at the active site of MAO-A enzyme by doing important interactions owing to the docking studies. Finally, ADME predictions were applied to estimate pharmacokinetic profiles of synthesized compounds. According to calculated ADME predictions, all parameters of the compounds were within the standard ranges in terms of Rule of Five and Rule of Three and it was detected that the synthesized compounds (2a-4i) have good and promising pharmacokinetic profiles.Publication Metadata only A new series of 1,3,4-oxadiazole derivatives: Synthesis and evaluation of antimicrobial activity(2021-11-12) TOK, FATİH; TOK F., ÖZARDA M. G.Aim: Infectious diseases have become more and more life-threatening illnesses. Despite a large number of antimicrobial agents, deaths due to infectious diseases are increasing day by day. Antimicrobial drugs have remained insufficiently against some infectious diseases caused outbreaks such as Zika, Ebola, SARS and MERS coronaviruses during the last decades. Therefore, new antimicrobial agents are urgently needed. 1,3,4-Oxadiazole ring is an important pharmacophoric group which is exhibited a broad spectrum of pharmacological activity profile including their antibacterial, antifungal, antiviral, antimalarial, antitubercular properties (1). In this study, we aimed the synthesis of new 1,3,4-oxadiazole rings and evaluation of their antimicrobial activity. Methods: New 2,5-disubstituted-1,3,4-oxadiazoles were synthesized at three steps. All compounds were characterized with spectral methods such as IR, 1H-NMR, 13C-NMR and elemental analysis. The antimicrobial activity of 1,3,4-oxadiazoles was screened on four bacteria and three fungi according to our previous method (2). Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus were used for antibacterial activity; Candida albicans, Candida parapsilosis and Candida glabrata were used for anticandidal activity. Results: Minimum inhibitory concentration (MIC) was determined for test compounds and for the reference standards chloramphenicol, ketoconazole. The compound carrying methoxy substituent on the para position of the aromatic ring exhibited the same antibacterial activity as chloramphenicol against E. faecalis with a MIC50 value of 62.50 µM/mL. Conclusions: According to the results, we demonstrated that some compounds exhibit antimicrobial activities against tested microorganisms. Therefore, the oxadiazole nucleus is promising for new drug candidates.Publication Metadata only Synthesis of novel pyrazoline derivatives carrying piperidine ring andinvestigation of their anticancer activities(2022-03-13) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; UĞRAŞ Z., TOK F., ŞALVA E., KAYMAKÇIOĞLU B.