- Synthesis and anticancer activity evaluation of N-[4-(2-methylthiazol-4-yl) phenyl]acetamide derivatives containing (benz)azole moiety
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A new class of novel thiazole-(benz)azole derivatives was synthesized to investigate their anticancer activity. The structure of the compounds was confirmed by IR, 1H-NMR, and MS spectral data and elemental analyses. Anticancer effect of the compounds was evaluated against A549 and C6 tumor cell lines. MTT, analysis of DNA synthesis, acridine orange/ethidium bromide staining method and analysis of caspase-3 activation assays were performed for anticancer activity investigations. Compounds 6f and 6g, which carry 5-chloro and 5-methylbenzimidazole groups showed significant anticancer activity. Potential of these compounds to direct tumor cells to apoptotic pathway, which is a precondition of anticancer action, was also observed.
- Yurtta?, Leyla,?zkay, Yusuf,Akalin-?ift?i, Gül?en,Ulusoylar-Yildirim, ?afak
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p. 175 - 184
(2014/04/03)
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- Synthesis, anticandidal activity, and cytotoxicity of some thiazole derivatives with dithiocarbamate side chains
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Some thiazole derivatives bearing dithiocarbamic acid esters were synthesized in order to investigate their anticandidal activity and cytotoxicity. The structures of the obtained final compounds (6a-j) were confirmed by spectral data (IR, 1H NMR, 13C NMR, and MS) and elemental analysis. The anticandidal activity of the compounds was determined (6a-j) using the microbroth dilution method and their cytotoxicity was evaluated according to the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against normal cells. Contrary to expectations, weak antifungal activity was observed with IC50values ranging between 30 and 403 μg/mL.
- Yurtta, Leyla,?zkay, Yusuf,?ztürk, ?mer,Kaplancikli, Zafer Asim,Demirci, Fatih,G?ger, Gamze,Ulusoylar Yildirim, afak,Abu Mohsen, Usama
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p. 815 - 824
(2014/12/10)
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- Synthesis and antimicrobial activities of novel series of 3-(4-(2-substituted thiazol-4-yl)phenyl)-2-(4-methyl-2-substituted thiazol-5-yl)thiazolidin-4-one derivatives
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In the present investigation, a novel series of 3-(4-(2-substituted thiazol-4-yl)phenyl)-2-(4-methyl-2-substituted thiazol-5-yl)thiazolidin-4-one derivatives were synthesized by condensation of 2-substituted-4-methylthiazole- 5-carbaldehyde with 4-(2-subs
- Shelke, Shivaji H.,Mhaske, Pravin C.,Narkhade, Sachin,Bobade, Vivek D.
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p. 1151 - 1156
(2014/08/05)
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- Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors
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In this study, some new 2-(4-substituted piperazine-1-yl)-N-[4-(2- methylthiazol-4-yl)phenyl]acetamide derivatives were synthesized. The synthesized compounds were screened for their anticholinesterase activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro Ellman's method. The structural elucidation of the compounds was performed by using IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses results. Biological assays revealed that at 0.1 μM concentration, the most active compounds against AChE were 5n, 5o and 5p that indicated 96.44, 99.83 and 89.70% inhibition rates, respectively. Besides, IC50 value of the compound 5o was determined as 0.011 μM, whereas IC50 value of standard drug donepezil was 0.054 μM. The synthesized compounds did not show any notable inhibitory activity against BChE.
- Yurttas, Leyla,Kaplancikli, Zafer Asim,Oezkay, Yusuf
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p. 1040 - 1047
(2013/10/01)
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- NOVEL 2,6-SUBSTITUTED-3-NITROPYRIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
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The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyr
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Page/Page column 12
(2012/01/03)
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- NOVEL 2,6-SUBSTITUTED-3-NITROPYRIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
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The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyr
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Page/Page column 18
(2012/01/03)
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- Synthesis and anticancer activities of some thiazole derivatives
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In this study, 2-substituted 4-[3/4-(4-arylthiazole-2-yl)aminophenyl] thiazole derivatives and 2-[4-[2-substituted 4-methylthiazole-5-yl]thiazole-2- yl]amino-5-arylidenethiazoline-4-one derivatives have been synthesized. The cytotoxic and/or growth inhibitory effects of the 16 selected compounds were evaluated in vitro against approximately 66 human tumor cell lines derived from nine neoplastic diseases. Some of the compounds were found to act as anticancer agents.
- Kayagil, Ismail,Demirayak, Seref
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scheme or table
p. 2197 - 2207
(2010/04/24)
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- Optically active antifungal azoles. X. Synthesis and antifungal activity of N-[4-(azolyl)phenyl]- and N-[4-(azolylmethyl)phenyl]-N′-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy -1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-azolones
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New optically active antifungal azoles, N-[4-(azolyl)phenyl]- and N-[4-(azolylmethyl)phenyl]-N′-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy -1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]azolones (1, 2, 3), were prepared in a stereocontrolled manner. Compounds 1
- Kitazaki, Tomoyuki,Ichikawa, Takashi,Tasaka, Akihiro,Hosono, Hiroshi,Matsushita, Yoshihiro,Hayashi, Ryogo,Okonogi, Kenji,Itoh, Katsumi
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p. 1935 - 1946
(2007/10/03)
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