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    Potassium carbonate mediated one-pot synthesis and antimicrobial activities of 2-alkoxy-4-(aryl)-5H-indeno[1,2b] pyridine-3-carbonitriles
    (ACG PUBLICATIONS, 2016) Ozturk, Sahin; Gurdere, Meliha Burcu; Gezegen, Hayreddin; Ceylan, Mustafa; Budak, Yakup
    2-Alkoxy-4-(aryl)-5H-indeno[ 1,2-b] pyridine-3-carbonitriles (3a-e and 4a-e) were synthesized via multicomponent reaction from 2-aryl-methylidineindan-1-ones (1a-e), malononitrile and K2CO3 in ethanol and/or methanol. The structures of obtained compounds (3a-e and 4a-e) were characterized using the spectroscopic methods (NMR, IR) and elemental analysis. Addition, the in vitro antimicrobial activities of compounds (3a-e) were tested against the five human pathogenic bacteria. Penicillin G and Ceftriaxone antibiotics were used as positive control. The results were given as MIC values (minimum inhibition concentration), and compounds 3b-d showed very high activity against Escherichia coli 111.
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    Purification of glutathione S-transferase enzyme from quail liver tissue and inhibition effects of (3aR,4S,7R,7aS)-2-(4-((E)-3-(aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives on the enzyme activity
    (WILEY, 2018) Temel, Yusuf; Kocyigit, Umit M.; Taysi, M. Serif; Gokalp, Faik; Gurdere, Meliha Burcu; Budak, Yakup; Ceylan, Mustafa; Gulcin, Ilhami; Ciftci, Mehmet
    The use of quail meat and eggs has made this animal important in recent years, with its low cost and high yields. Glutathione S-transferases (GST, E.C.2.5.1.18) are an important enzyme family, which play a critical role in detoxification system. In our study, GST was purified from quail liver tissue with 47.88-fold purification and 12.33% recovery by glutathione agarose affinity chromatography. The purity of enzyme was checked by SDS-PAGE method and showed a single band. In addition, inhibition effects of (3aR,4S,7R,7aS)-2-(4-((E)-3-(aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7methanoisoindole-1,3(2H)-dion derivatives (1a-g) were investigated on the enzyme activity. The inhibition parameters (IC50 and K-i values) were calculated for these compounds. IC50 values of these derivatives (1a-e) were found as 23.00, 15.75, 115.50, 10.00, and 28.75M, respectively. K-i values of these derivatives (1a-e) were calculated in the range of 3.04 +/- 0.50 to 131.50 +/- 32.50M. However, for f and g compounds, the inhibition effects on the enzyme were not found.
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    Synthesis and investigation of antibacterial activities and carbonic anhydrase and acetyl cholinesterase inhibition profiles of novel 4,5-dihydropyrazol and pyrazolyl-thiazole derivatives containing methanoisoindol-1,3-dion unit
    (TAYLOR & FRANCIS INC, 2017) Budak, Yakup; Kocyigit, Umit M.; Gurdere, Meliha Burcu; Ozcan, Kezban; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
    Novel 4,5-dihydropyrazole derivatives (3a-i), 3-(4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothio amide, were obtained by the addition of thiosemicarbazide (2) to the chalcones (1a-i). The addition-cyclization of 2,4-dibromoacetophenone (4) to pyrazole derivatives (3a-i) gave the new pyrazolyl-thiazole derivatives (5a-i), (3aR,4S,7R,7aS)-2-(4-(1-(4-(4-bromophenyl)thiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione. Antibacterial and acetylcholinesterase (AChE) enzyme and human carbonic anhydrase (hCA) I, and II isoform inhibitory activities of the compounds 3a-i and 5a-i were investigated. Some of the compounds showed promising antibacterial activity. In addition, the hCA II and I were effectively inhibited by the lately synthesized derivatives, with K-i values in the range of 18.90 +/- 2.37 -58.25 +/- 13.62nM for hCA II and 5.72 +/- 0.98 -37.67 +/- 5.54nM for hCA I. Also, the K-i parameters of these compounds for AChE were obtained in the range of 25.47 +/- 11.11-255.74 +/- 82.20nM. Also, acetazolamide, clinical molecule, was used as a CA standard inhibitor that showed K-i value of 70.55 +/- 12.30nM against hCA II, and 67.17 +/- 9.1nM against hCA I, and tacrine inhibited AChE showed K-i value of 263.67 +/- 91.95. [GRAPHICS] .
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    Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones
    (SPRINGER WIEN, 2019) Kocyigit, Umit M.; Budak, Yakup; Gurdere, Meliha Burcu; Duru, Nese; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
    A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with K-i values in the range of 3.33-7.90nM for hCA I and 2.07-8.47nM for hCA II, while the K-i values of these compounds for AChE were recorded in the range of 9.61-48.42nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest K-i values to make further detailed CA inhibition studies. [GRAPHICS] .
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    Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles
    (TAYLOR & FRANCIS LTD, 2018) Kocyigit, Umit Muhammet; Budak, Yakup; Gurdere, Meliha Burcu; Erturk, Fatih; Yencilek, Belkiz; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
    The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 mu M. IC50 value of 5-fluorouracil (5-FU) was 90.36 mu M. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 +/- 227.4nM against CA I, and 904.47 +/- 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 +/- 58.33 nM.
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    Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives
    (Wiley-V C H Verlag Gmbh, 2020) Gurdere, Meliha Burcu; Aydin, Ali; Yencilek, Belkiz; Erturk, Fatih; Ozbek, Oguz; Erkan, Sultan; Budak, Yakup
    Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives with IC(50)values of 86-168 mu M demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5-fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (similar to 6 nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1x103 M-1-2.3x104 M-1. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.
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    Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives
    (ACADEMIC PRESS INC ELSEVIER SCIENCE, 2017) Kocyigit, Umit M.; Budak, Yakup; Gurdere, Meliha Burcu; Tekin, Saban; Koprulu, Tugba Kul; Erturk, Fatih; Ozcan, Kezban; Gulcin, Ilhami; Ceylan, Mustafa
    In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl) acryloyl) phenyl)-3a, 4,7,7a-tetrahydro-1H-4,7-methanoisoin dole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80.51-97.02% compared to 5-FU. Some of the compounds exhibited anti-microbial activity. Also, they evaluated for inhibition effects against human carbonic anhydrase I, and II isoenzymes (hCA I and II) with Ki values in the range of 405.26-635.68 pM for hCA I, and 245.40-489.60 pM for hCA II, respectively. These results demonstrated that 3aR, 4S, 7R, 7aS)-2-(4-((E)-3-(3-aryl) acryloyl) phenyl)-3a, 4,7,7a-tetrahy dro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives could be used in different biomedical applications. (C) 2016 Elsevier Inc. All rights reserved.