- Basic N-interlinked imipramines show apoptotic activity against malignant cells including Burkitt's lymphoma
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We here report the synthesis of ethylene glycol N-interlinked imipramine dimers of various lengths from the tricyclic antidepressant desipramine via an amide coupling reaction followed by reduction with lithium aluminium hydride. The target molecules were found to be potent inhibitors of cellular viability while inducing cell type specific death mechanisms in three cancer cell lines including a highly chemoresistant Burkitt's lymphoma cell line. Basic amine analogues were found to be important for increased potency. Imipramine and desipramine were also tested for apoptotic activity and were found to be much less active than the novel dimeric compounds. Imipramine dimers were only found to be moderate inhibitors of the human serotonin transporter (hSERT) having IC50 values in the micromolar region whilst the induction of cell death occurred independently of hSERT expression. These results demonstrate the potential of newly designed and synthesised imipramines derivatives for use against malignant cells, including those resistant to standard chemotherapy.
- Bright, Sandra A.,Brink?, Anne,Larsen, Maja Thim,Sinning, Steffen,Williams, D. Clive,Jensen, Henrik H.
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- Ether acid cobalt complex single crystal and preparation method as well as application thereof
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The invention discloses ether acid cobalt complex single crystal, having a structure of [Co(L)(H2O)], wherein L is equal to di-ethoxy di-acetic acid. The invention also discloses a preparation method of the single crystal. According to the preparation method, a normal temperature volatilization method is adopted, i.e., L and Co(Ac)2.H2O are stirred in water for half an hour, and then are filtered, and filtrate is volatilized at normal temperature for two weeks, thus obtaining red blocky crystal suitable for X-ray single crystal diffraction, wherein the mol ratio of Co(Ac)2.H2O is 1 to 1. The invention further discloses application of the ether acid cobalt complex single crystal as a potential fluorescent material in detection on the adsorption quantity of a dye or an illuminating agent.
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Paragraph 0018; 0019
(2016/12/01)
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- Ligand Recognition by E- and P-Selectin: Chemoenzymatic Synthesis and Inhibitory Activity of Bivalent Sialyl Lewis x Derivatives and Sialyl Lewis x Carboxylic Acids
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Described is the preparation of five sLex dimers and five sLex carboxylic acids by coupling chemoenzymatically synthesized amino-substituted sialyl Lewis x (sLex) derivative 4 to homobifunctional cross-linkers 20-24 of varying chain length. 20-24 were obtained by alkylating low-molecular-weight oligoethylene glycols with tert-butyl bromoacetate and subsequent transformation of the di-tert-butyl esters into disuccinimide esters. The products were assayed for inhibition against binding of a sLea-polymer to immobilized E- and P-selectin. In the E-selectin assay all dimers had lower IC50 values than the sLex monomer. The results show that comparable binding enhancements can be obtained with linkers of completely different length and rigidity. In the P-selectin assay four of the five sLex carboxylic acids displayed significantly improved inhibitory potency. The lowest IC50 value was observed for the compound with the shortest spacer between the sLex moiety and the additional carboxylate, being ca. 20-40 times more potent than unmodified sLex. These findings should be of importance for the design of new multivalent forms of sLex as well as sLex mimetics as high-affinity selectin ligands.
- Wittmann, Valentin,Takayama, Shuichi,Gong, Ke Wei,Weitz-Schmidt, Gabriele,Wong, Chi-Huey
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p. 5137 - 5143
(2007/10/03)
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- CHIRAL AMINOACID CONTAINING ACYCLIC LIGANDS-I. SYNTHESES AND CONFORMATIONS
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Synthesis and spectral properties of optically active acyclic ligands, containing two (S)-phenylalanine residues (3a-f) are described.The synthesis is achieved by two different routes.Conformational studies in different solvents are performed by dilution and temperature-dependent experiments of 1H and 13C NMR spectroscopy.
- Lodi, T.,Marchelli, R.,Dossena, A.,Dradi, E.,Casnati, G.
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p. 2055 - 2060
(2007/10/02)
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- OXIDATION OF ALCOHOLS BY ELECTROCHEMICALLY REGENERATED NICKEL OXIDE HYDROXIDE. SELECTIVE OXIDATION OF HYDROXYSTEROIDS
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Primary alcohols, α,ω-diols and secondary alcohols are easily transformed into carboxylic acids, dicarboxylic acids or ketones, respectively, by heterogeneous oxidation with nickel oxide hydroxide electrochemically regenerated at a nickel hydroxyde electrode.The results are discussed in comparison to those of the nickel peroxide and chromic acid oxidation.The oxidation rate decreases with increasing steric hindrance of the alcohol, thus allowing the selective oxidation of the 3-position in hydroxysteroids.
- Kaulen, Johannes,Schaefer, Hans-J.
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p. 3299 - 3308
(2007/10/02)
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- Complexes of macrocyclic compounds
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Novel macrocyclic (monocyclic and bicyclic) compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.
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- Process for preparing di(alkoxy-carboxy) hydrocarbylenes
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A process for preparing di(alkoxycarboxy) hydrocarbylenes which comprises contacting carbon monoxide with a saturated aldehyde and a non-adjacent dihydric alcohol in the presence of a catalytic amount of hydrogen fluoride.
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