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Design, synthesis and evaluation of d-galactose-beta-cyclodextrin conjugates as drug-carrying molecules

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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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Brief introduction of 2-(2-Chloroethoxy)tetrahydro-2H-pyran

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BROMODOMAIN TARGETING DEGRONIMERS FOR TARGET PROTEIN DEGRADATION

This invention provides a Degronimer that has an E3 Ubiquitin Ligase targeting moiety (Degron) that can be linked to a Targeting Ligand for a bromodomain protein selected for in vivo degradation to achieve a therapeutic effect, and methods of use and compositions thereof as well as methods for their preparation.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Awesome Chemistry Experiments For 2-(2-Chloroethoxy)tetrahydro-2H-pyran

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Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors

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,
Tetrahydropyran – an overview | ScienceDirect Topics

Some scientific research about 2-(2-Chloroethoxy)tetrahydro-2H-pyran

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Synthesis and Characterization of Large (30-60-Membered) Aliphatic Crown Ethers

We report a new synthetic approach to large (30-72 membered) crown ethers based on isolation of the small and large cyclic polyethers made by combination of 1 mol or 2 mol each, respectively, of oligo(ethylene glycol)s and oligo(ethylene glycol) ditosylates.The advantages of this approach are the use of readily available glycols as starting materials and the ability to optimize the procedure for selective production of either macrocycle, producing yields superior or comparable to previous methods.At higher reaction temperatures the large crown ether is preferentially formed.This approach has been used to produce the crown ethers on 100-g scales.Purification was achieved by a combination of filtration through silica gel, treatment with a polymeric acid chloride, and recrystallization techniques, avoiding standard column chromatography.The pure crown ethers, 60-crown-20, 48-crown-16, 42-crown-14, 36-crown-12, and 30-crown-10, were characterized by melting points, 1H- and 13C-NMR, elemental analysis, and/or MS, GC-MS, and TGA-MS.Melting points were as much as 26 deg C higher than previously reported for these crown ethers.All the aliphatic crown ethers larger than 18-crown-6 decompose upon heating in air at ca. 200 deg C.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Properties and Exciting Facts About 5631-96-9

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5631-96-9, Name is 2-(2-Chloroethoxy)tetrahydro-2H-pyran, molecular formula is C7H13ClO2. In a Patent£¬once mentioned of 5631-96-9, Application In Synthesis of 2-(2-Chloroethoxy)tetrahydro-2H-pyran

Pharmaceutical compounds

A pharmaceutical compound of the formula STR1 and salts and esters thereof.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The important role of 2-(2-Chloroethoxy)tetrahydro-2H-pyran

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 5631-96-9 is helpful to your research., Synthetic Route of 5631-96-9

Synthetic Route of 5631-96-9, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 5631-96-9, Name is 2-(2-Chloroethoxy)tetrahydro-2H-pyran, molecular formula is C7H13ClO2. In a Patent£¬once mentioned of 5631-96-9

A nitrogen-containing heterocyclic derivatives and their application in the retinal disease (by machine translation)

The invention discloses a nitrogen-containing heterocyclic derivatives and their application in the retinal disease, nitrogen-containing heterocyclic derivatives is the formula Wherein R1 , R2 , R3 , R4 Independently selected from – H or – F. 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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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Brief introduction of 5631-96-9

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Azepino [1,2,3-lm]-beta-carboline compounds and pharmaceutical composition thereof

An azepino[1,2,3-lm]-beta-carboline compound of the formula: STR1 wherein R1 is hydrogen, cycloalkyl of 3 to 7 carbon atoms, phenyl, hydroxy, alkoxycarbonyl of 2 or 3 carbon atoms or alkanoyl of 2 or 3 carbon atoms, and A is single bond or straight or branched alkylene of one to 5 carbon atoms. Several methods of preparing the compound [I] are disclosed. The compound [I] and a pharmaceutical acceptable acid addition salt thereof have a potent anti-anoxic activity.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Brief introduction of 2-(2-Chloroethoxy)tetrahydro-2H-pyran

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PROCEDURE FOR PREPARING A PHARMACEUTICALLY ACTIVE COMPOUND

The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Discovery of 5631-96-9

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Chromoionophores, VII. Podands Carrying Terminal Electron-Donor- and -Acceptor Groups. Cation-Influenced Charge Transfer Absorption

The synthesis and spectroscopic investigation of the new noncyclic neutral ligands 12-20 of the glycol ether type (podands) carrying terminal electron-donor- and -acceptor groups are described.The podands show intramolecular charge transfer interactions which can be influenced selectively by complexed cations.The ligands 13 and 20 cause significant increases of extinction and bathochromic shifts of the charge transfer bands in the UV/Vis spectra on addition of alkali perchlorates, whereas the shorter ligands 14 and 18 show a decrease of extinction and hypsochromic shifts under similar conditions.Some of the noncyclic chromoionophores discern considerably and visually perceivably between Na+ and K+ or Li+ and Na+, respectively, in acetonitrile.The cation selective alterations in the electron spectra are discussed in view of steric effects considering some complex stability constants determined by photometric titrations.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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The treatment of HIV-1 infection using certain pyridodiazepines

Disclosed are novel pyridodiazepines. These compounds, as well certain known 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics