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    Antiproliferative Evaluation of Some 2-[2-(2-Phenylethenyl)-cyclopent-3-en-1-yl]-1,3-benzothiazoles: DFT and Molecular Docking Study
    (Wiley-V C H Verlag Gmbh, 2020) Ceylan, Mustafa; Erkan, Sultan; Yaglioglu, Ayse Sahin; Uremis, Nuray Akdogan; Koc, Esra
    The 2-[2-(2-phenylethenyl)cyclopent-3-en-1-yl]-1,3-benzothiazoles were synthesized from the reactions of 7-benzylidenebicyclo[3.2.0]hept-2-en-6-ones with 2-aminobenzenethiol. The antiproliferative activities of 2-[2-(2-phenylethenyl)cyclopent-3-en-1-yl]-1,3-benzothiazoles were determined against C6 (rat brain tumor) and HeLa (human cervical carcinoma cells) cell lines using BrdU cell proliferation ELISA assay. Cisplatin and 5-fluorouracil (5-FU) were used as standards. The most active compound was 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against C6 cell lines with IC50=5.89 mu m value (cisplatin, IC50=14.46 mu m and 5-FU, IC50=76.74 mu m). Furthermore, the most active compound was 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against HeLa cell lines with IC50=3.98 mu m (cisplatin, IC50=37.95 mu m and 5-FU, IC50=46.32 mu m). Additionally, computational studies of related molecules were performed by using B3LYP/6-31G+(d,p) level in the gas phase. Experimental IR and NMR data were compared with the calculated results and were found to be compatible with each other. Molecular electrostatic potential (MEP) maps of the most active 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against HeLa and the most active 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against C6 were investigated, aiming to determine the region that the molecule is biologically active. Biological activities of mentioned molecules were investigated with molecular docking analyses. The appropriate target protein (PDB codes: 1 M17 for the HeLa cells and 1JQH for the C6 cells) was used for 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole and 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole molecules exhibiting the highest biological activity against HeLa and C6 cells in the docking studies. As a result, it was determined that these molecules are the best candidates for the anticancer drug.
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    Synthesis, characterization and antiproliferative activities of novel modified poly (maleic anhydride-co-vinyl acetate)/cytosine beta-D-arabinofuranoside hydrochloride conjugate
    (MARMARA UNIV, FAC PHARMACY, 2015) Karakus, Gulderen; Yaglioglu, Ayse Sahin; Zengin, Haci Bayram; Karakus, Nihat
    Poly (maleic anhydride-co-vinyl acetate) (MAVA) copolymer was synthesized by free-radical-polymerization reaction in methyl ethyl ketone (MEK) at 80 degrees C using benzoyl-peroxide (BPO) as the radical-initiator. MAVA was then modified with anti-leukemic chemotherapy-agent cytosine beta-D-arabinofuranoside hydrochloride (CF). Modification was performed at 70 degrees C in dimethylformamide (DMF) containing triethylamine (Et3N) as the catalyst. Structural characterization of the copolymer and copolymer/drug couple (MAVA/CF) was carried out by Fourier Transform Infrared (FTIR) and Nuclear Magnetic Resonance (H-1-NMR). FTIR and H-1-NMR spectra confirmed the modification reaction. UV-Spectrophotometric measurements indicated that MAVA/CF kept its molecular integrity in physiological-body-fluid, PBS, for first four days. Antiproliferative activities of MAVA/CF were also determined by BrdU-cell-proliferation-ELISA assays using C6 and HeLa cell lines (cisplatin and 5-fluorouracil used as positive control). MAVA/CF appeared to have little antiproliferative activity against C6 cell line while samples didn't have antiproliferative activity against HeLa cell line at low concentrations (<100 mu g/ml). Reaction mechanism was also recommended for modification product MAVA/CF.
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    Synthesis, characterization, and assessment of cytotoxic, antiproliferative, and antiangiogenic effects of a novel procainamide hydrochloride-poly(maleic anhydride-co-styrene) conjugate
    (TAYLOR & FRANCIS LTD, 2013) Karakus, Gulderen; Polat, Zubeyde Akin; Yaglioglu, Ayse Sahin; Karahan, Mesut; Yenidunya, Ali Fazil
    Poly(maleic anhydride-co-styrene) (MAST) was synthesized by a free-radical polymerization reaction. A bioactive molecule, procainamide hydrochloride (PH), was then conjugated to MAST. The conjugation product was named as MAST/PH. Structural characterization of MAST and MAST/PH was carried out by Fourier Transform Infrared and Nuclear Magnetic Resonance spectroscopy. Their molecular weights were determined by size-exclusion chromatography. A mechanism was then suggested for the conjugation reaction. The results of the cytotoxicity assay, employing a mouse fibroblast cell line (L929), indicated that MAST/PH had no cytotoxicity at concentrations 62gmL(1) (p>0.05). Antiproliferative activities of MAST/PH and PH were determined by the BrdU cell proliferation ELISA assay, using C6 and HeLa cell lines. In the experiment, two anticancer chemotherapy drugs, cisplatin and 5-fluorouracil, were included as positive control. Antiproliferative activity results demonstrated that MAST/PH yielded the highest suppression profile (approximately 42%) at 20g/ml, while free PH exerted the same activity at 100g/ml. Interestingly, both MAST/PH and PH suppressed the proliferation of only one of the cell lines, C6 cells. Both cisplatin and 5-fluorouracil yielded approximately 60% antiproliferative activity on C6 cells at 20 and 100g/ml concentrations. Antiangiogenic capacity of both MAST and MAST/PH was also investigated by using the chicken chorioallantoic membrane assay. Results obtained indicated that while MAST/PH could be included into the category of good antiangiogenic substances, the activity score of MAST was within the weak category.
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    Synthesis, structural characterization, and antiproliferative/cytotoxic effects of a novel modified poly(maleic anhydride-co-vinyl acetate)/doxorubicin conjugate
    (SPRINGER, 2017) Karakus, Gulderen; Ece, Abdulilah; Yaglioglu, Ayse Sahin; Zengin, Haci Bayram; Karahan, Mesut
    Drug carrier, poly(maleic anhydride-co-vinyl acetate) (MAVA or poly[MA-co-VA]) copolymer, was traditionally synthesized by free radical chain polymerization reaction, in methyl ethyl ketone (MEK) organic media at 80 A degrees C, using benzoyl peroxide (BPO) as the radicalic initiator. The purified copolymer was then modified with a chemotherapeutic agent, doxorubicin hydrochloride (DOX) at 75 A degrees C for 72 h, using N-(3-dimethyl-aminopropyl)-N'-ethylcarbodiimide hydrochloride (EDAC) as the carboxylic acid-activating agent. Structural characterization of the MAVA and the modified MAVA/DOX conjugate was carried out by Fourier transform infrared (FTIR) and nuclear magnetic resonance (H-1-NMR and C-13-NMR). Their molecular weights were determined by size-exclusion chromatography (SEC). The spectroscopic and SEC results confirmed that conjugated/modification reaction was successfully carried out. UV spectrophotometric measurements indicated that MAVA/DOX preserved its molecular stability in physiological body fluid, PBS (physiological pH 7.40 at 37 A degrees C). Antiproliferative activities of MAVA/DOX were determined by BrdU cell proliferation ELISA assay using C6 (Rat Brain tumor cells) and HeLa (human uterus carcinoma) cell lines in vitro by comparing with free DOX agent (reference compound). Although MAVA showed low antiproliferative activity, both MAVA/DOX and DOX exhibited greater activity against HeLa and C6. Lactate dehydrogenase (LDH) leakage assay was performed for MAVA/DOX and DOX, which detected a non-toxic effect against C6 even at the highest dose (100 mu g/mL). IC50 and IC75 values were also determined using ED50 plus v1.0. Molecular modeling at M06-L/6-31 + G(d,p)//AM1 level showed that the electron density in MAVA/DOX is more localized resulting a higher polarization and thereby a higher dipole moment which shed light on the solubility of MAVA/DOX conjugate.
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    Synthesis, structural characterization, thermal behavior and cytotoxic/antiproliferative activity assessments of poly(maleic anhydride-alt-acrylic acid)/hydroxyurea polymer/drug conjugate
    (Elsevier, 2020) Karakus, Gulderen; Can, Hatice Kaplan; Yaglioglu, Ayse Sahin
    As drug carrier, poly(maleic anhydride-alt-acrylic acid) copolymer [poly(MA-alt-AA)], was prepared traditionally by radical initiated (benzoyl peroxide (BPO)), complex-radical polymerization technique via charge transfer complex (CTC) (50/50 in p-dioxane, at 70 degrees C under a nitrogen atmosphere). The pure alternating carrier was then conjugated as poly[MA-alt-AA]/HX (or MAAA/HX) copolymer/drug couple by ring opening reaction with an antineoplastic agent hydroxyurea (HX) for 48 h at 75 +/- 0.1 degrees C in dimethylformamide (DMF), presence of triethylamine (Et3N) catalytic base. Chemical structure of the copolymer, antineoplastic agent and conjugate was characterized by Fourier Transform Infrared (ATR-FTIR) and also Nuclear Magnetic Resonance (proton and carbon NMR). Physical characterizations were also carried out by Thermogravimetric Analysis (TGA) and Differential Scanning Calorimetry (DSC). To verify the elemental composition and also conjugation reaction of conjugated product, quantitative elemental analysis was especially carried out. Cytotoxicity was determined with Lactate Dehydrogenase (LDH) leakage assay using LDH cytotoxicity detection kit provided by Roche Diagnostics GMBH (Mannheim, Germany) based on the protocol in the user's manual. Compared with 5-FU, toxicity values are as follows respectively: HX > MAAA > 5-FU. MAAA/HX. Furthermore, antiproliferative activity studies was examined on HeLa (human cervical cancer) and (C6) rat brain tumor cells using proliferation BrdU ELISA assay. Conjugated-drug was identified to have the higher antiproliferation than the copolymer and free-drug (Hydroxyurea) on all studied concentrations and cellular potency of inhibitions were found as MAAA/HX > HX > MAAA at the highest concentration, 100 mu g/mL. Toxic drug (HX) was modified as nontoxic MAAA/HX conjugate with good properties. (C) 2020 Elsevier B.V. All rights reserved.