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11.
Mirjana Popsavin Vesna Kojić Saša Spaić Miloš Svirčev Gordana Bogdanović Dimitar Jakimov Lidija Aleksić Velimir Popsavin 《Tetrahedron》2014
Tiazofurin analogues bearing a 5-hydroxymethyl-2-methyl-tetrahydrofuro[2,3-d][1,3]dioxol-6-ol moiety as a sugar mimic (2 and 3), and two novel thiazole-based acyclo-C-nucleosides 4 and 16 have been synthesized in multistep sequences starting from d-xylose (compounds 2 and 3) or from d-arabinose (compounds 4 and 16). All synthesized analogues showed potent in vitro antitumour activities against a panel of human tumour cell lines. Flow cytometry data suggest that cytotoxic effects of analogues 2–4 and 16 in the culture of K562 cells might be mediated by apoptosis. It was also found that these analogues induced changes in cell cycle distribution of K562 cells. Results of western blot analysis (upregulation of Bax and downregulation of Bcl-2, activation of caspase-3 and the presence of a PARP cleavage product) suggest that tiazofurin mimics (2–4 and 16) in K562 cells induced apoptosis in a caspase-dependent way. 相似文献
12.
Milena Simic Predrag Jovanovic Milos Petkovic Gordana Tasic Milos Jovanovic Vladimir Savic 《Journal of heterocyclic chemistry》2021,58(8):1665-1674
Octahydro-dipyrroloquinoline skeleton is the building component of a very few naturally occurring compounds. Nevertheless, these natural products have been attractive synthetic targets, and their study commanded development of efficient synthesis of this core. While the reported methods are based on the dimerization procedure of N-arylpyrrolidines of N-arylhomopropargyl amines, our approach relay on dipolar cycloaddition/amination sequence. This strategic approach allows sequential introduction of aromatic moieties increasing the product diversity and hence may be useful in further exploration of incargranine B or seneciobipyrrolidine derivatives. 相似文献
13.
Luljeta Raka Andrea Sorrentino Gordana Bogoeva‐Gaceva 《Journal of Polymer Science.Polymer Physics》2010,48(17):1927-1938
The effect of organo‐modified clay (Cloisite 93A) on the crystal structure and isothermal crystallization behavior of isotactic polypropylene (iPP) in iPP/clay nanocomposites prepared by latex technology was investigated by wide angle X‐ray diffraction, differential scanning calorimetry and polarized optical microscopy. The X‐ray diffraction results indicated that the higher clay loading promotes the formation of the β‐phase crystallites, as evidenced by the appearance of a new peak corresponding to the (300) reflection of β‐iPP. Analysis of the isothermal crystallization showed that the PP nanocomposite (1% C93A) exhibited higher crystallization rates than the neat PP. The unfilled iPP matrix and nanocomposites clearly shows double melting behavior; the shape of the melting transition progressively changes toward single melting with increasing crystallization temperature. The fold surface free energy (σe) of polymer chains in the nanocomposites was lower than that in the PP latex (PPL). It should be reasonable to treat C93A as a good nucleating agent for the crystallization of PPL, which plays a determinant effect on the reduction in σe during the isothermal crystallization of the nanocomposites. The activation energy, ΔEa, decreased with the incorporation of clay nanoparticles into the matrix, which in turn indicates that the nucleation process is facilitated by the presence of clay. © 2010 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 48: 1927–1938, 2010 相似文献
14.
Pavlović SZ Belić D Blagojević DP Radojicić RM Zikić RV Saicić ZS Grubor-Lajsić G Spasić MB 《Cryo letters》2004,25(4):273-285
The activity of cytosolic antioxidative defence enzymes in the liver and white muscle of thinlip gray mullet (Liza ramada Risso) were compared in winter and spring in the Adriatic Sea. Activity of antioxidative enzymes is functionally organized due to metabolic demands: analyses of variance and correlation analysis revealed tissue- and seasonal- specific organization of antioxidative enzymes. In winter GST activity increased in both tissues compared with spring. At the same time decreased GSH-Px and GR activities were observed and this effect was more pronounced in liver then in white muscle. From correlation analyses it is concluded that the antioxidative components correlate, but the composition of the antioxidative defence system is different in respect to season and tissue. This means that the antioxidative defence system reorganizes its structure due to oxidative demands and to protect the tissues against reactive oxygen species and to establish homeostasis. Discriminant analyses separated groups according to the complete organization of individual components of the system very well and identified individual components (CAT, GST and GR) which contribute most to the differences. Statistical differences were observed between enzyme activities in tissues (liver and muscle) in both winter and spring, and between seasons (winter and spring) for liver tissue only. Since environmental parameters, such as temperature and oxygen concentration in the sea differ with season, we conclude that in this species the tissues examined expressed their antioxidative defence systems in different ways in respect of external/environmental conditions. We propose that tissue- and seasonal- specific levels of antioxidant enzyme activities should be considered in the interpretation of data from future biomonitoring field studies, especially in relation to low temperature. 相似文献
15.
Luljeta Raka Gordana Bogoeva-Gaceva Joachim Loos 《Journal of Thermal Analysis and Calorimetry》2010,100(2):629-639
The extent of organo-modified clay (C93A) platelets dispersion in polymer matrix and crystallization and melting behavior
of iPP-based nanocomposites prepared by a single-step melt-mixing method were investigated by wide-angle X-ray diffraction
(WAXD), transmission (TEM), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC). WAXD patterns
revealed exfoliated structure of nanocomposites containing 1 wt% clay, and mixed intercalated/exfoliated structure at higher
concentration of nanoclay. The isothermal crystallization proceeds faster in the matrix polymer (iPP/PP-g-MA) than in nanocomposite samples. The results obtained for T
m
o suggest that the presence of nanoclay has induced a perfection of the formed crystals. The presence of C93A particles in
PP leads to increase in crystallization peak temperature implying nucleating ability of clay particles, which was more pronounced
in exfoliated than in mixed intercalated/exfoliated system. 相似文献
16.
Abstract
In order to investigate the intramolecular [4 + 2] cycloaddition, we prepared some new tertiary N-(5-substituted-2-furfuryl)-N-prop-2-ynyl-p-toluidines [Hergold-Brundić et al., Acta Cryst C56:e520, 2000; Mance and Jakopčić, Mol Divers 9:229, 2005; Mance, “unpublished results”] by the alkylation of secondary N-(5-substituted-2-furfuryl)-p-toluidines with the propargyl-bromide [Mance and Šindler-Kulyk, Synth Commun 26:923, 1996]. In the course of preparation of N-(5-methoxy-2-furfuryl)-N-prop-2-ynyl-p-toluidine [Mance, “unpublished results”], besides the main product (compound 1) (Scheme 1) we obtained N,N-di(prop-2-ynyl)-p-toluidine (compound 2) as the colourless crystals. The title compound 2, N,N-di(prop-2-ynyl)-p-toluidine, C13H13N, crystallizes in monoclinic C 2/c space group with unit cell parameters: a = 19.5319(9) ?, b = 7.5230(3) ?, c = 15.9000(7) ?, β = 112.554(5)°, V = 2157.64(18) ?3, Z = 8. The crystal structure is dominated by van der Waals forces only. The bond distances around amine N atom correspond to σ dominated bonds (1.467(2), 1.462(2) and 1.419(2) ?). The angles sum around amine N atom is in accord with sp3 hybridization (343°). 相似文献17.
JPC – Journal of Planar Chromatography – Modern TLC - The behavior of 5,5-disubstituted hydantoin derivatives has been studied using four chromatographic systems, two normal-phase... 相似文献
18.
Snezana Savic Gordana Vuleta Rolf Daniels Christel C. Müller-Goymann 《Colloid and polymer science》2005,283(4):439-451
The aim of this study was to examine the lyotropic potential of an alkylpolyglucoside mixed emulsifier (Cetearyl glucoside&Cetearyl alcohol), which belongs to the new generation of natural (sugar) surfactants, and to elaborate the potential stabilization mechanism and relation between the colloid microstructure and water distribution within the systems. Polarization and ordinary light as well as transmission electron microscopy, wide and small-angle X-ray diffraction, thermal analysis and rheological measurement were employed for the systems characterization.It was suggested that Cetearyl glucoside&Cetearyl alcohol stabilizes the o/w creams by synergistic effects of viscoelastic hydrophilic gel of lamellar type and lipophilic gel network built up from cetostearyl alcohol semi-hydrates as well as by lamellar liquid crystalline bilayers surrounding the oil droplets. The hydrophilic gel consists of mixed cetearyl glucoside/cetearyl alcohol crystalline bilayers entrapping the water interlamellarly by hydrogen bonding. It is also showed that oil addition into the chosen binary system influences the creams microstructure significantly, which particularly reflects onto the mode of water distribution within the creams and consequently their potential of skin hydration. 相似文献
19.
The spatial inhomogeneity of pulsed atmospheric pressure discharge in argon is investigated using the electron number density Ne diagnostics procedure applied to asymmetrically broadened Ar I lines. A dedicated fitting procedure is used for describing Ar I 703.0 nm line shape recorded from argon gas discharge and H I (at 486.13 and 656.28 nm) lines recorded from Ar-H2 gas mixture discharge. The results revealed the change in Ne in both axial and radial directions. The additional Ar I lines at 614.5, 710.7, 731.2, and 731.6 nm, recorded from integral spatial radiation, are analysed as well to confirm the results from the plasma column region. The possibility of using AlO (B2∑+–X2∑+) and CN (B2∑+–X2∑+) molecular bands for gas temperature Tg measurements in this type of gas discharge source is demonstrated and Tg used as an input parameter for the Ne diagnostics procedure. For the proper identification of molecular band spectral lines, the Fortrat parabolas are constructed. The results obtained from Ar I 703.0 nm line indicate three different Ne values, with Ne1 ≈ 0.6 × 1016 cm−3, Ne2 ≈ 3.6 × 1016 cm−3, and Ne3 ≈ 19 × 1016 cm−3 measured from the plasma column. These Ne values increase in the cathode and anode region. 相似文献
20.
Mirjana Popsavin Miloš Svir?evLjilja Torovi? Gordana Bogdanovi?Vesna Koji? Dimitar JakimovSaša Spai? Lidija Aleksi?Velimir Popsavin 《Tetrahedron》2011,67(36):6847-6858
Synthesis of four new tiazofurin analogues has been accomplished starting from d-glucose. The key step of the synthesis was the three-step cascade that enabled an efficient hydrogen sulfide mediated one-pot conversion of 2-azido-3-O-acyl-ribofuranosyl cyanides to the corresponding 2-alkylamido ribofuranosyl thiocarboxamides. The resulting key intermediates were first converted to protected tiazofurin derivatives by cyclocondensation with ethyl bromopyruvate, and finally to target C-nucleosides by treatment with ammonia in methanol. In vitro cytotoxicities of tiazofurin analogues against a number of human tumour cell lines were recorded and compared with those observed for the parent molecule (tiazofurin), as well as the commercial antitumour agent doxorubicin (DOX). Analogues 2b-d have shown a potent in vitro cytotoxic activity against human myelogenous leukaemia K562. Among solid tumour cell lines, HT29 was sensitive only to 2d, while HeLa cells were sensitive to 2a, 2b and 2d. Only analogue 2a was highly cytotoxic against MCF-7 cells. No tiazofurin analogue exhibits any significant cytotoxicity towards normal foetal lung MRC-5 cells. Downregulation of Bcl-2, activation of caspase-3 and presence of cleavage product of PARP suggest that the cytotoxic effects of tiazofurin analogues 2a-d in K562 might be mediated by apoptosis in a caspase-dependent way. On the contrary, tiazofurin did not induce apoptosis of K562 cells, which suggests a different mechanism of action, most probably through the inhibition of IMPDH. Flow cytometry and Western blot analysis data agreed well with the results of MTT assay, and enabled identification of analogue 2c as the most promising antitumour agent that preferentially target cancer cells over normal cells and thus represents a new lead for further optimization. 相似文献