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  • 1
    Keywords: APOPTOSIS ; CANCER ; CELLS ; ANTITUMOR-ACTIVITY ; POTENT ; POLO-LIKE KINASE ; SMALL-MOLECULE INHIBITOR ; SELECTIVE INHIBITOR ; POLO-LIKE-KINASE-1 ; BI-2536
    Abstract: We synthesized a series of vanillin-derived compounds and analyzed them in HeLa cells for their effects on the proliferation of cancer cells. The molecules are derivatives of the lead compound SBE13, a potent inhibitor of the inactive conformation of human polo-like kinase 1 (Plk1). Some of the new designs were able to inhibit cancer cell proliferation to a similar extent as the lead structure. Two of the compounds ((({4-[(6-chloropyridin-3-yl)methoxy]-3-methoxyphenyl}methyl)(pyridin-4-ylmethyl) amine) and (({4-[(4-chlorophenyl)methoxy]-3-methoxyphenyl}methyl)(pyridin-4-ylmethyl)amine)) were much stronger in their capacity to reduce HeLa cell proliferation and turned out to potently induce apoptosis and reduce Plk1 kinase activity in vitro.
    Type of Publication: Journal article published
    PubMed ID: 25304894
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  • 2
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    German Medical Science GMS Publishing House; Düsseldorf
    In:  43. Kongress der Deutschen Gesellschaft für Rheumatologie (DGRh); 29. Jahrestagung der Deutschen Gesellschaft für Orthopädische Rheumatologie (DGORh); 25. wissenschaftliche Jahrestagung der Gesellschaft für Kinder- und Jugendrheumatologie (GKJR); 20150902-20150905; Bremen; DOCRA.38 /20150901/
    Publication Date: 2015-09-02
    Keywords: ddc: 610
    Language: German
    Type: conferenceObject
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Acta mechanica 6 (1968), S. 42-55 
    ISSN: 1619-6937
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Description / Table of Contents: Summary The plane self-equilibrating state of stress is investigated, which originates in an infinitely long circular cylinder of isotropic linear-elastic but discontinuously inhomogeneous material, if the latter is subjected to a plane non-steady temperature distribution. Applying complex function analysis and avoiding series developments an approximate solution of this nonhomogeneous thermal stress problem can be constructed which satisfies all boundary conditions exactly. The transition conditions are also satisfied exactly at every point of the interface with the exception of they-component of the displacement vector. For a special case the exact solution—theAiry surfaceF(x, y)—can be given in closed form.
    Notes: Zusammenfassung Es wird ein ebener Eigenspannungszustand untersucht, der sich in einem unendlich langen Kreiszylinder isotropen linear-elastischen aber diskontinuierlich inhomogenen Materials ausbildet, wenn letzteres einer ebenen unstetigen Temperaturverteilung unterworfen wird. Bei Verwendung der komplexen Analysis und unter Vermeidung von Reihenentwicklungen kann eine Näherungslösung dieses inhomogenen Temperaturspannungsproblems konstruiert werden, die die Randbedingungen exakt erfüllt. Die Übergangsbedingungen werden bis auf diejenige für diey-Komponente des Verschiebungsvektors für jeden Punkt der Diskontinuitätsfläche exakt erfüllt. Für einen Spezialfall läßt sich die exakte Lösung—dieAirysche FlächeF(x, y)—in geschlossener Form angeben.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1619-6937
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-203X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The dihydrofuroacridone, rutacridone, is the main alkaloid in tissue cultures of Ruta graveolens L. strain R-19. The biosynthesis of this particular acridone alkaloid was investigated by using calluses and suspension cultures of strain R-19. Anthranilic acid is specifically incorporated into ring A of rutacridone. Some further evidence was provided that acetate via a polyketide is involved in acridone biosynthesis. Mevalonic acid gave a poor incorporation into rutacridone. Thus the origin of the isopropyldihydrofuran moiety of the investigated alkaloid is still obscure.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 0138-4988
    Keywords: Life Sciences ; Life Sciences (general)
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Process Engineering, Biotechnology, Nutrition Technology
    Notes: Two isoenzymes of chorismate mutase (EC 5.4.99.5), designated as CM-1 and CM-2, were isolated and partially purified from suspension-cultured cells of Ruta gravelens by DEAE-sephacel chromatography and gel filtration. 60-72% of the total activity measured after DEAE-sephacel chromatography were obtained as CM-1 and 28-40% were CM-2 activity. CM-1 was inhibited by phenylalanine (K1 = 4 · 10-6 M) and tyrosine (K1 = 8. 10-6M) and activated by tryptophan. In contrast, CM-2 was not influenced by these three amino acids. The molecular weights estimated by gel filtration on SEPHADEX G-150 were 56000 for CM-1 and 45000 for CM-2, respectively. Both isoenzymes were stable at -20°C, but exhibited different behaviour during thermal inactivation and different optima of reaction temperature. CM-1 catalysed the reaction at a pH optimum of pH 7.8 and CM-2 showed a broad optimum between 6-10. The Km-values for chorismic acid were determined to be 1.1 mM for CM-1 and 0.5 mM for CM-2. The isoenzymes showed different behaviour to inhibitors of sulfhydryl groups. There were no differences in all parameters of chorismate mutase examined for two various cell lines of Ruta graveolens.
    Additional Material: 8 Ill.
    Type of Medium: Electronic Resource
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