Person: KAYMAKÇIOĞLU, BEDİA
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KAYMAKÇIOĞLU
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BEDİA
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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 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 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 Pirazolon halkasından hareketle sentezlenen çeşitli Schiff bazları üzerinde saflaştırmaçalışmaları(2018-11-16) TOK, FATİH; KAYMAKÇIOĞLU, BEDİA; Yılmaz S., TOK F., KAYMAKÇIOĞLU B.Publication Metadata only Synthesis, anticancer activity and ADMET studies of N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido] benzenesulfonamide derivatives(TAYLOR & FRANCIS LTD, 2018) KAYMAKÇIOĞLU, BEDİA; Karakus, S.; Tok, F.; Tuerk, S.; Salva, E.; Tatar, G.; Taskin-Tok, T.; Kocyigit-Kaymakcioglu, B.A series of novel 4-[(3-substituted)ureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamides and 4-[(3-substituted)thioureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamides were prepared from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide (sulfamethizole). The structures of the synthesized compounds were determined by IR, H-1-NMR, MS and elemental analysis. The anticancer activity of these compounds was evaluated against human colorectal carcinoma (HCT116) and human cervix carcinoma (HeLa) cell lines. Compound 4 (4-{[(2,4-dichlorophenyl)carbamoyl]amino}-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide) showed marked anticancer activity, being the most active compounds in this series with the IC50 value of 13.92 +/- 0.22 mu M and 37.91 +/- 0.10 mu M against HeLa and HCT116, respectively. In silico, ADMET was used to examine their pharmacokinetic properties. ADMET (absorption, distribution, metabolism, excretion, and toxicity) studies were applied to develop new anticancer compound(s) with high selectivity. [GRAPHICS] .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 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.