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  1. Ana Sayfa
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Yazar "Sivas, H." seçeneğine göre listele

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    Anticancer activities of African medicinal spices and vegetables
    (Academic Press Ltd-Elsevier Science Ltd, 2017) Kuete, V.; Karaosmanoğlu, Oğuzhan; Sivas, H.; Kuete, V
    …
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    Theoretical and experimental electronic transition behaviour study of 2-((4-(dimethylamino) benzylidene)amino) -4-methylphenol and its cytotoxicity
    (Elsevier B.V., 2020) Uysal, U.D.; Ercengiz, D.; Karaosmanoğlu, Oğuzhan; Berber, B.; Sivas, H.; Berber, H.
    In this study, a Schiff base (2-((4-(dimethylamino)benzylidene)amino)-4-methylphenol; 7S2) has been synthesized and characterized with 1H, 13C-NMR, IR and elemental analysis methods. An electronic transition behaviour of the Schiff base has been investigated in the different eight solvents by UV-Vis. spectroscopy. The stable geometry of 7S2 has been determined by DFT method with Gaussian09 program (B3LYP/6-311G(2d, p)). 7S2 has been analysed for its target region selection using the SwissTarget program. A docking study has been performed against DHODH protein while its pharmacokinetic properties has been evaluated using SwissADME, Osiris and Molinspiration. 7S2 has important pharmacokinetic and drug-likeness properties against other FDA approved DHODH inhibitors. Further, 7S2 has been tested with the neutral red uptake assay and found cytotoxic for several cancer cell lines, having IC50 values ranged between 18-23 µg/mL. According to the pharmacokinetic properties and cytotoxic activities, we suggest that 7S2 may have a potential as an anticancer drug. © 2020 Elsevier B.V.
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    Two new pterocarpans and a new pyrone derivative with cytotoxic activities from Ptycholobium contortum (N.E.Br.) Brummitt (Leguminosae): Revised NMR assignment of mundulea lactone
    (BioMed Central Ltd., 2016) Ngnintedo, D.; Fotso, G.W.; Kuete, V.; Nana, F.; Sandjo, L.P.; Karaosmanoğlu, Oğuzhan; Sivas, H.
    Background: Ptycholobium is a genus related to Tephrosia which comprises only three species. Compared to Tephrosia, which has been phytochemically and pharmacologically studied, Ptycholobium species have only few or no reports on their chemical constituents. Moreover, no studies on the cytotoxic activities of its secondary metabolites have been previously documented. Results: From the non polar fractions of the roots bark of Ptycholobium contortum (syn Tephrosia contorta), two new pterocarpans: seputhecarpan C 1 and seputhecarpan D 2 and a new pyrone derivative, ptycholopyrone A 3 were isolated. Alongside, five known compounds identified as 3-?,?-dimethylallyl-4-methoxy-6-styryl-?-pyrone or mundulea lactone 4, glyasperin F 5, seputhecarpan A 6, seputheisoflavone 7 and 5-O-methyl-myo-inositol or sequoyitol 8 were also obtained. Their structures were established by the mean means of spectroscopic data in conjunction to those reported in literature. The NMR assignment of the major compound mundulea lactone 4 is revised in this paper. In addition, the cytotoxicity of the isolated metabolites was evaluated on two lung cancer cell lines A549 and SPC212. 8 was not active while compounds 1, 2, 4-7 displayed antiproliferative effects against the two carcinoma cell lines with IC50 values below 75 ?M. IC50 values below 10 ?M were obtained for 4, 6 and 7 on SPC212 cells. Conclusion: Based on the obtained results, Ptycholobium contortum turns to be a rich source of phenolic metabolites among them some bearing prenyl moieties. This study reports for the first time the isolation of pyrone derivatives 3 and 4 from Ptycholobium genus. The cytotoxicity observed for the isolate is also reported for the first time and shows that 4, 6 and 7 could be chemically explored in order to develop a hit candidate against lung cancer. © 2016 The Author(s).

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