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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Recommanded Product: 17402-83-4, C8H7NS. A document type is Patent, introducing its new discovery., Recommanded Product: 17402-83-4

Provided are a pyrimidinyl amino compound having protein kinase inhibitor activity, and a pharmaceutical composition containing said compound; also provided are a use and application of said compound. What is provided is selected from a group consisting of the compound represented by formula (I), a stereoisomer thereof, a tautomer thereof, a pharmacologically acceptable salt thereof, a solvate thereof, and a prodrug thereof. The described compound has good inhibitory activity against the JAK family of kinases and the SYK family of kinases, and therefore may serve as a JAK inhibitor and SYK inhibitor, and is effective in use for the prevention or treatment of diseases related to the JAK and SYK families of kinases.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Background Pyridoquinazolinecarboxamides have been reported as RNA polymerase I inhibitors and represent a novel class of potential antitumor agents. BMH-21, was reported to intercalate with GC-rich rDNA, resulting in nucleolar stress as a primary mechanism of cytotoxicity. Methods The interaction of BMH-21 and analogues with DNA G-quadruplex structures was studied by NMR and molecular modelling. The cellular response was investigated in a panel of human tumor cell lines and protein expression was examined by Western Blot analysis. Results and conclusions We explored the ability of BMH-21 and its analogue 2 to bind to G-quadruplex present in the c-MYC promoter, by NMR and molecular modelling studies. We provide evidence that both compounds are not typical DNA intercalators but are effective binders of the tested G-quadruplex. The interaction with c-MYC G-quadruplex was reflected in down-regulation of c-Myc expression in human tumor cells. The inhibitory effect was almost complete in lymphoma cells SUDHL4 characterized by overexpression of c-Myc protein. This downregulation reflected an early and persistent modulation of cMyc mRNA. Given the relevance of c-MYC in regulation of ribosome biogenesis, it is conceivable that the inhibition of c-MYC contributes to the perturbation of nuclear functions and RNA polymerase I activity. Similar experiments with CX-5461, another RNA polymerase I transcription inhibitor, indicate the same behaviour in G-quadruplex stabilization. General significance Our results support the hypothesis that BMH-21 and analogue compounds share the same mechanism, i.e. G-quadruplex binding as a primary event of a cascade leading to inhibition of RNA polymerase I and apoptosis.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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New Advances in Chemical Research in 2021. Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, new energy materials, preparation and modification of special coatings. 4923-87-9. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

The functionalization of thiophenes is a fundamental and important reaction. Herein, we disclose iridium-catalyzed one-pot annulation reactions of (benzo)thiophenes with (hetero)aromatic or alpha,beta-unsaturated carboxylic acids, which afford thiophene-fused coumarin-type frameworks. Dearomatization reactions of 2-substituted thiophenes with alpha,beta-unsaturated carboxylic acids deliver various thiophene-containing spirocyclic products. The occurrence of two interconnected reactions provides direct evidence for a Heck-type pathway. The mechanistic scenario described herein is distinctly different from the SEAr and concerted metalation?protodemetalation (CMD) pathways encountered in the well-described oxidative C?H/C?H cross-coupling reactions of thiophenes with other heteroarenes.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.

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New Advances in Chemical Research, May 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and transition states. Quality Control of 4-Chlorobenzo[b]thiophene, C8H5ClS. A document type is Patent, introducing its new discovery., Quality Control of 4-Chlorobenzo[b]thiophene

The invention provides a piripiprazole derivative and a preparation method, wherein the chemical structural formula of the epiprazole derivative is expressed by a chemical structural formula. The epiprazole derivative is composed of epiconazole, (HCHO). m N – hydroxymethyl according to the first basic catalyst is prepared; and then N – hydroxymethyl-piripiprazole and an alkylformylchloride compound are reacted under second basic catalyst to prepare. The half-life of the epiprazole derivative is prolonged, the drug delivery frequency can be reduced; and the epiprazole derivative prepared by the preparation method is low in impurity, and low in cost. (by machine translation)

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More research is needed about C10H7BrO2S

The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about 360576-01-8

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Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

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Benzothiophene – Wikipedia,
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New Advances in Chemical Research in 2021. Catalysts allow a reaction to proceed that has a lower activation energy than the uncatalyzed reaction. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Application In Synthesis of 5-Bromobenzothiophene. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

The present invention relates to a novel indole-based compound having excellent hole injection and transport capabilities, light-emission, and other properties, and to an organic electroluminescent device the luminous efficiency, driving voltage, service life, and other characteristics of which are improved due to containing the compound in one or more organic material layers.

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 130-03-0. In my other articles, you can also check out more blogs about 130-03-0

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The kinetics of the hydronium-ion catalysed hydrolysis of the following heterocyclic methyl enol ethers have been measured: 3-methoxybenzofuran, 3-methoxybenzothiophene, 3-methoxyindole, 3-methoxy-1-methylindole, 3-methoxyfuran, 3-methoxythiophene, and 2-methoxythiophene.On the basis of the solvent isotope effect kH/kD = 3.08 and the failure to detect deuterium exchange when the solvent was CD3CN:D2O (9:1 v/v) it was concluded that the rate limiting step in the hydrolysis of 3-methoxybenzofuran is C-protonation.The effect of the ring-oxygen atom was measured by comparing the rate of hydrolysis of 3-methoxybenzofuran with that of 3-methoxyindene which occurs 2100 times faster.In contrast to the behaviour of 3-methoxybenzofuran the isotope effects, kH/kD, for the hydrolyses of 3-methoxyfuran, 3-methoxythiophene, 3-methoxyindole, 3-methoxy-1-methylindole and 2-methoxythiophene are ca 0.4 – 0.5 and deuterium exchange is much faster than hydrolysis when the solvent is CD3CN:D2O (9:1 v/v).It was therefore concluded that with these compound C-protonation is rapid and reversible and that slow step is attack by water on the intermediate cation.

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Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

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Reference:
Benzothiophene – Wikipedia,
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In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of y2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the y2C adrenergic receptors using such compounds or pharmaceutical compositions.

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Benzothiophene – Wikipedia,
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