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Bismuth trichloride as mild reagent, has been found to be a worthful catalyst for tetrahydropyranylation of 1,2,3, allylic, benzylic alcohols, and symmetric di-ols. At room temperature the reagent THP(3,4-dihydro-2H-pyran) was successfully employed as pyranylating agent in presence of BiCl3catalyst without the use of a solvent and the yields of the products were found to be 90-96%. Further, the depyranylation of alcohols was achieved in quantitative yield by simple addition of MeOH using the same catalyst. The developed method was showed good chemo-selectivity in symmetrical diols for mono THP protection.

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The canonical WNT pathway plays an important role in cancer pathogenesis. Inhibition of poly(ADP-ribose) polymerase catalytic activity of the tankyrases (TNKS/TNKS2) has been reported to reduce the Wnt/beta-catenin signal by preventing poly ADP-ribosylation-dependent degradation of AXIN, a negative regulator of Wnt/beta-catenin signaling. With the goal of investigating the effects of tankyrase and Wnt pathway inhibition on tumor growth, we set out to find small-molecule inhibitors of TNKS/TNKS2 with suitable drug-like properties. Starting from 1a, a high-throughput screening hit, the spiroindoline derivative 40c (RK-287107) was discovered as a potent TNKS/TNKS2 inhibitor with >7000-fold selectivity against the PARP1 enzyme, which inhibits WNT-responsive TCF reporter activity and proliferation of human colorectal cancer cell line COLO-320DM. RK-287107 also demonstrated dose-dependent tumor growth inhibition in a mouse xenograft model. These observations suggest that RK-287107 is a promising lead compound for the development of novel tankyrase inhibitors as anticancer agents.

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Tetrahydropyran – Wikipedia,
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Several kinds of d-galactose-beta-cyclodextrin conjugates having a phenyl group in the spacers between the d-galactose and beta-cyclodextrin were designed and synthesized as drug-carrying molecules. Their evaluation as drug-carrying molecules was done by measuring the molecular interactions with the anticancer agent, doxorubicin, and with the d-galactose-binding peanut lectin using an SPR optical biosensor. The SPR analyses showed that these conjugates had remarkably high inclusion associations of 105 ? 107 M-1 levels for the immobilized doxorubicin. Their association constants for immobilized peanut lectin were at the level of 104 ? 105 M-1, as we expected. These conjugates will be useful drug-carrying models which can site-specifically carry doxorubicin to the cells containing d-galactose-binding lectin.

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The invention discloses a nitrogen-containing heterocyclic derivatives and their angiogenesis diseases of the retina in the application, the nitrogen-containing heterocyclic derivatives is the formula Wherein R1 , R2 , R3 , R4 Independently selected from – H or – CN. In the 5 mug/mL under the same concentration, the implementation of the example two, implementation […] HRCEC […] and implementation of growth inhibition rate of the superior to the monoclonal antibody medicine Avastin. To the intravitreal injection after administration, the compounds of the invention can reduce the pathological neovascularization, illustrate the invention nitrogen-containing heterocyclic […] I or the salts thereof can be used for the treatment of retinal angiogenesis related diseases in-depth research and development, the diseases such as retinal vein occlusion, shelter for diabetic retinopathy, retinal new blood vessel membrane, neovascular glaucoma, premature retinopathy, such as proliferative vitreoretinopathy. (by machine translation)

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 5631-96-9, Name is 2-(2-Chloroethoxy)tetrahydro-2H-pyran, molecular formula is C7H13ClO2. In a Patent,once mentioned of 5631-96-9, Recommanded Product: 5631-96-9

The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions. Yet another aspect of the invention is to provide methods for treating or preventing diseases, particularly viral infections and cell growth disorders. The subject disease treatment methods comprise the step of administering an effective amount of the subject polynucleotide analogs for use as antisense inhibitors.

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Synthetic routes to forty-four dibenzocrown ether alcohols are reported. The new crown ether compounds are based on a sym-dibenzo-16-crown-5 platform. Most have a hydroxy group and an alkyl, aryl, aralkyl, alkenyl, alkynyl, or perfluoroalkyl group on the central carbon of the three-carbon bridge. Others have substituted benzene rings and either a hydroxy or -O(CH2)(n) OH group attached to the central carbon of the three-carbon bridge.

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Efficient routes for the synthesis of norbornadiene-tethered nitrones have been developed and their intramolecular 1,3-dipolar cycloadditions were found to be highly regio- and stereo-selective.

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The chemoselective one-pot conversion of tetrahydropyranyl (THP) and methoxymethyl (MOM) ethers of primary alcohols to the corresponding acetates was presented. It was done using indium triiodide-catalysed deprotection and subsequent acetylation by ethyl acetate through a transesterification process. The advantages offered by the method included operational simplicity, ‘green’ methodology involving no toxic or hazardous chemicals and high yield.

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This study discusses the synthesis of two new 2-hydroxyethyl substituted N-heterocyclic carbene (NHC) precursors. The NHC precursors were prepared from 1-(alkyl/aryl)benzimidazole and alkyl halides. They were characterized using 1H NMR, 13C NMR, FT-IR, UV?Vis spectroscopy, and elemental analysis techniques. Molecular and crystal structures of 1 and 2 were determined using the single-crystal X-ray diffraction method. Crystal structure of the compounds features NHC precursors and chloride anions. Additionally in 2, the asymmetric unit has a water molecule, which forms a tetrameric chloride-hydrate assembly with the chloride anion. The chloride anions play an important role in the stabilization of crystal structures to form a two-dimensional supramolecular architecture. The 3D Hirshfeld surface and the associated 2D fingerprint plots were also drawn to gain insights into the behavior of the interactions in the compounds.

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Four deuterium-labelled neoglycolipids derived from cholesterol were synthesized for embedment into liposomes. Deuterium atoms were either incorporated by CH2 replacement with a CD2 group in the triethylene glycol spacer arm between the cholesteryl residue and the sugar moiety (products 2-4) or incorporated directly on the acetamido function in the sugar head (compound 5). Copyright

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Reference:
Tetrahydropyran – Wikipedia,
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