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31.
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   
32.
The separation of structurally related angiotensin-converting enzyme (ACE) inhibitors lisinopril, cilazapril, ramipril and quinapril and their corresponding active diacid forms (prilates) by conventional TLC silica gel 60 plates was contrasted with that afforded by monolithic ultra-thin-layer chromatographic (UTLC) plates. For the use of UTLC plates technical modifications of the commercially available equipments for the sample application, development and detection were made. Plates were developed in modified horizontal developing chamber using ethyl acetate-acetone-acetic acid-water (4:1:0.25:0.5, v/v). Detection of the separated compounds was performed densitometrically in absorption/reflectance mode at 220 nm and after exposure to iodine also by image analysis. The obtained results showed that monolithic layer is more efficient for the separation of structurally similar polar compounds, such as prilates than conventional silica layers. Identification of the compounds was confirmed by ESI-MS after their on-line extraction from the UTLC and TLC plates by means of Camag TLC-MS interface.  相似文献   
33.
Associated with a finite-dimensional algebra of global dimension at most 2, a generalized cluster category was introduced in Amiot (2009) [1]. It was shown to be triangulated, and 2-Calabi–Yau when it is Hom-finite. By definition, the cluster categories of Buan et al. (2006) [4] are a special case. In this paper we show that a large class of 2-Calabi–Yau triangulated categories, including those associated with elements in Coxeter groups from Buan et al. (2009) [7], are triangle equivalent to generalized cluster categories. This was already shown for some special elements in Amiot (2009) [1].  相似文献   
34.
Cyclic posets are generalizations of cyclically ordered sets. In this article, we show that any cyclic poset gives rise to a Frobenius category over any discrete valuation ring R. The stable category of a Frobenius category is always triangulated and has a cluster structure in many cases. The continuous cluster categories of [14 Igusa , K. , Todorov , G. ( 2013 ). Continuous Frobenius categories . Proceedings of the Abel Symposium 2011 : 115143 .[Crossref] [Google Scholar]], the infinity-gon of [12 Holm , T. , Jøot rgensen , P. ( 2012 ). On a cluster category of infinite Dynkin type, and the relation to triangulations of the infinity-gon . Math. Z. 270 : 277295 .[Crossref], [Web of Science ®] [Google Scholar]], and the m-cluster category of type A (m ≥ 3) [13 Holm , T. , Jøot rgensen , P. ( 2015 ). Cluster tilting vs. weak cluster tilting in Dynkin type A infinity . Forum Math. 27 : 11171137 .[Crossref], [Web of Science ®] [Google Scholar]] are examples of this construction as well as some new examples such as the cluster category of ?2. An extension of this construction and further examples are given in [16 Igusa, K., Todorov, G. Continuous Cluster Categories of Type D. arXiv:1309.7409 . [Google Scholar]].  相似文献   
35.
Plasma of argon stabilized arc column, in a current range 3-11 A, is investigated using emission spectrometric diagnostic techniques. Temperatures are evaluated using several methods: argon line to adjacent recombinational continuum intensity ratio, absolute emissivity of argon line, measurement of electron number density, and power interruption. Electron number density is evaluated from absolute emissivity of recombinational continuum. The difference between electron Te and heavy particle Th temperature ranged from 4500 K for 3 A to 2300 K for 11A arc current. By comparing the present with the previously obtained results, using the same arc device but with the introduction of water aerosol, it is concluded that water aerosol reduces the difference Te - Th and brings plasma closer to the partial thermodynamic equilibrium state.  相似文献   
36.
During metal welding and cutting, large amounts of particulate matter (PM) are produced that might represent a significant health risk for the exposed workers. In the present pilot study, we performed an elemental analysis of fine PM collected in a metal workshop. Also, elemental analysis of the hair and nail samples collected from workers exposed to the workshop dust and control group was done. Concentrations of 15 elements in PM were measured with X‐Ray Fluorescence (XRF) and Particle Induced X‐ray Emission (PIXE), whereas inductively coupled plasma mass spectrometry (ICP‐MS) was used to determine 12 elements in hair and nail samples. Mean 8‐hr concentrations of PM2.5, Fe, and Mn in the vicinity of welders were up to 1803, 860, and 30 μg/m3, respectively, whereas in the nearby city, daily PM2.5 concentrations are on average 11 μg/m3. We found that several elements, especially Fe and Mn, had substantially higher concentrations in hair and nail samples of exposed workers than in the control group, which indicates the accumulation of metals in workers' tissues, although limit values were not exceeded.  相似文献   
37.
Triangulated categories coming from cyclic posets were originally introduced by the authors in a previous paper as a generalization of the constructions of various triangulated categories with cluster structures.We give an overview, and then analyze "triangulation clusters" which are those corresponding to topological triangulations of the 2-disk. Locally finite nontriangulation clusters give topological triangulations of the "cactus space" associated to the "cactus cyclic poset".  相似文献   
38.
A one-pot, domino process was developed as an alternative approach for the preparation of 2-unsubstituted imidazolones. The methodology utilizes readily accessible bisamides, which upon a dehydration/cyclisation sequence produced imidazolones in good yields. The transformation relies on the compatibility of the dehydrating agent and base, and the reaction conditions tolerate various functional groups.  相似文献   
39.
The authors report on a novel sorbent (thermally treated natural zeolite; clinoptilolite) for use in dispersive micro-solid phase extraction (D-μ-SPE) of polycyclic aromatic hydrocarbons (PAHs) from water samples. The method was applied to the D-μ-SPE of 16 priority PAHs which then were quantified by gas chromatography with mass spectrometric detection (GC-MS). The method was validated in terms of specificity and selectivity, linearity and linear range, accuracy, precision, uncertainty, limits of detection and quantification. Figures of merit include (a) linear analytical ranges between 2.08 and 208 ppb, and (b) detection limits in the range from 0.01 to 0.92 ppb. The method was successfully applied to the determination of PAHs in river waters.
Graphical abstract Schematic representation of dispersive micro-solid phase extraction (D-μ-SPE) of trace levels of PAHs in water samples by using thermally treated clinoptilolite as sorbent prior to gas chromatography-mass spectrometry analysis (GC-MS).
  相似文献   
40.
Phytochemical analysis by GC and GC/MS of the essential oil samples obtained from fresh shoots and flowers of Saponaria officinalis L. allowed the identification of 96 components in total, comprising 94.7% and 86.0% of the total oils compositions, respectively. Regarding the shoots essential oil, the major of 87 identified volatile compounds were phytol (14.1%), tricosane-6,8-dione (13.4%), patchouli alcohol (7.9%) and tricosane (7.2%), whereas patchouli alcohol (20.0%), heneicosane (11.5%) and tricosane (8.4%) were dominant among the 66 volatiles in the flower oil. Nonterpenoid compounds had the highest contribution in S. officinalis shoots essential oil (53.7%), while in the flower oil, constituents were almost evenly distributed between the oxygenated sesquiterpenoid (41.2%) and nonterpenoid compounds (39.5%).  相似文献   
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