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    Antimicrobial and cytotoxic studies of new 2-substitue-1H-benzimidazole derivatives [Yeni 2-sübstitüe-1H-benzimidazol türevi bileşikler üzerinde antimikrobiyal ve sitotoksik çali{dotless}şmalar]
    (University of Istanbul, 2011) Sarikaya G.; Alpan A.S.; Taşli H.; Sevin G.; Korkmaz C.G.; Güneş H.S.
    We synthesized a series of 2-substituted-1H-benzimidazole derivatives (1-9) of which six of them were original and elucidated their structures by spectral analyses. We also evaluated the in-vitro antimicrobial activities of the synthesized compounds and detected potent inhibitory action in some of the compounds. Moreover, 2-(1H-benzimidazole-2-yl)phenol intermediates, bearing o-hydroxyphenyl substituent on 1H-benzimidazole ring possess equal or similar results compared to the standard compound, Ceftazidime. The synthesized compounds didn't show any significant antifungal activity on Candida albicans. All nine 1H-benzimidazole derivatives were tested for their cytotoxicity through WST-1 colorimetric assay-based in vitro tests on the mammalian LNCaP cell line. Compounds 7 and 8 were found to have IC50 values of 0,09 ± 0,01 µM and 0,03 ± 0,02 µM, respectively. It is noteworthy that the values obtained with these two compounds were highly comparable to that of Doxorubicine 0,053 ± 0,003 µM, the reference drug used in our study.
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    Biological activity of bis-benzimidazole derivatives on DNA topoisomerase i and HeLa, MCF7 and A431 cells
    (Informa Healthcare, 2009) Alpan A.S.; Zencir S.; Zupkó I.; Coban G.; Rthy B.; Gunes H.S.; Topcu Z.
    Benzimidazoles of both natural and synthetic sources are the key components of many bio-active compounds. Several reports have shown antifungal, antiviral, H2 receptor blocker and antitumor activities for benzimidazoles and their derivatives. In this study, we synthesized twelve bis-benzimidazole derivatives by selecting di(1H-benzo[d]imidazol-2-yl)methane as the main compound. The numbers of carbons at 2 positions of bis-benzimidazole derivatives were changed from 1 to 4, and derivatives were synthesized with methyl substitutions at 5- and/or 6- positions. The compounds were screened via in vitro plasmid superciol relaxation assays using mammalian DNA topoisomerase I and cytostatic assays were carried out against HeLa (cervix adenocarcinoma), MCF7 (breast adenocarcinoma) and A431 (skin epidermoid carcinoma) cells for selected derivatives. Our results suggest that the malonic acid derivatives of bis-benzimidazoles, namely, bis(5-methyl-1H-benzo[d]imidazol-2-yl)methane and bis(5,6-dimethyl-1H-benzo[d] imidazol-2-yl)methane, were remarkably active compounds in interfering with DNA topoisomerase I and the former compound was also found to be cytotoxic against MCF7 and A431 cells. The inhibitory effects obtained with these derivatives are significant as these compounds can be potential sources of anticancer agents. © 2009 Informa UK Ltd.
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    Synthesis and voltammetric detection of 1H-benzimidazole derivatives on the interaction with DNA [1H-Benzimidazol türevlerinin sentezi ve DNA ile etkileşimlerinin voltametrik tayini]
    (2012) Alpan A.S.; Yilmaz Ö.; Kiliçkaya O.; Kara P.; Güneş H.S.; Özsöz M.Ş.
    In this study, synthesis and determination of interaction between DNA and 1H-benzimidazole derivatives has been performed by using electrochemical genosensor technology. Detection of DNA - drug interaction mechanism relies on monitoring Differential pulse voltammetric (DPV) responses of drugs at disposable graphite electrodes (DGEs). Interaction of 7 different benzimidazole derivates between double-stranded (ds) and singlestranded (ss) DNA were observed by changing the voltammetric signals of drugs at the detection limits of 0.62 nM of compound 1, 1.23 nM of 2, 1.26 nM of 3, 1.08 nM of 4, 1.13 nM of 5, 0.69 nM of 6 and 0.42 nM of 7, respectively.
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    Synthesis, antimicrobial activity and interaction with DNA of some 2-substituted benzimidazole derivatives
    (2009) Alcil P.; Alpan A.S.; Taşli H.; Yalçin G.; Güneş S.
    In this study, synthesis and structural illumination of eight compounds that are expected to display antifungal and antibacterial activity in addition to interaction with DNA has been conducted. The syntheses were performed by heating o-phenylendiamine and derivatives with succinic acid and malonic acid in 4N HCl. It has been observed that, the reactions with succinic acid formed bisbenzimidazole derivatives. On the other hand, the reactions with the malonic acid under the same conditions resulted in formation of benzimidazole derivatives instead of bisbenzimidazole derivatives. The structures of all synthesized compounds were analysed with spectroscopic methods (UV, IR, 'H NMR, MS). Among the synthesized compounds, 1 and 5 which are nonsubstitue compounds, were selected so as to dispose the roles of electron acceptor or donor atoms in the activity and their interaction with DNA has been examined with respect to concentration and time. When these two compounds were compared, it's seen that 1 requires higher concentrations and longer time to be able to interact with DNA. In addition, all compounds have been examined for antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Enterococcus faecalis, and for antifungal activities against Candida albicans. It was found that 7 was the most effective compound against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus, 5 was the most effective compound against Enterococcus faecalis, 7 and 8 were effective equivalently against Candida albicans.