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The reactions of ethyl (5-carbamoyl-3H-imidazol-4-yl)dithiocarbamate with phenacyl bromides afford the S-alkylation products as a mixture of E/Z-isomers, which undergo cyclization to 5-(2-oxo-4-arylthiazol-3-yl)-1H-imidazole-4-carboxamides under the action of a base.  相似文献   
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A series of novel S-, O- and Se-containing dispirooxindole derivatives has been synthesized using 1,3-dipolar cycloaddition reaction of azomethine ylide generated from isatines and sarcosine at the double C=C bond of 5-indolidene-2-chalcogen-imidazolones (chalcogen was oxygen, sulfur or selenium). The cytotoxicity of these dispiro derivatives was evaluated in vitro using different tumor cell lines. Several molecules have demonstrated a considerable cytotoxicity against the panel and showed good selectivity towards colorectal carcinoma HCT116 p53+/+ over HCT116 p53−/− cells. In particular, good results have been obtained for LNCaP prostate cell line. The performed in silico study has revealed MDM2/p53 interaction as one of the possible targets for the synthesized molecules. However, in contrast to selectivity revealed during the cell-based evaluation and the results obtained in computational study, no significant p53 activation using a reporter construction in p53wt A549 cell line was observed in a relevant concentration range.  相似文献   
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The following result is proved: Let D and D′ be bounded domains in ℂ n , ∂D is smooth, real-analytic, simply connected, and ∂D′ is connected, smooth, real-algebraic. Then there exists a proper holomorphic correspondence f:DD′ if and only if there exist points p∈∂D and p′∈∂D′, such that ∂D and ∂D′ are locally CR-equivalent near p and p′. This leads to a characterization of the equivalence relationship between bounded domains in ℂ n modulo proper holomorphic correspondences in terms of local CR-equivalence of their boundaries. Oblatum 23-I-2002 & 18-XI-2002?Published online: 17 February 2003  相似文献   
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LetM, M′ be smooth, real analytic hypersurfaces of finite type in ℂn and a holomorphic correspondence (not necessarily proper) that is defined on one side ofM, extends continuously up toM and mapsM to M′. It is shown that must extend acrossM as a locally proper holomorphic correspondence. This is a version for correspondences of the Diederich-Pinchuk extension result for CR maps.  相似文献   
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The kinetics of the reactions of ozone with 12 substituted olefins in aqueous solutions at 293 K are studied by the stopped-flow method. Second-order rate constants are determined for these reactions. The dependence of the reactivity of olefins in H2O on their structure can be described by the Taft equation.  相似文献   
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By hydrogenation of (20R,22R)-6α,14α,25-trihydroxy-and (20R,22R)-6β,14α,25-trihydroxy-2,3:20,22-bis(isopropylidenedioxy)-5α-cholest-7-enes on a catalyst (Raney nickel) the corresponding (5α,6α)-and (5β,6β)-epimers of previously unknown Δ8,14-6-hydroxy derivatives of ecdysteroids were synthesized.  相似文献   
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It is proved that CR functions on a quadratic cone M in , n > 1, admit one-sided holomorphic extension if and only if M does not have two-sided support, a geometric condition on M which generalizes minimality in the sense of Tumanov. A biholomorphic classification of quadratic cones in is also given.  相似文献   
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