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4-PYRIMIDINEAMINE COMPOUNDS AND THEIR USES AS ANTI-PROLIFERATIVE AGENTS

The present invention provides 4-pyrimidineamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Multicomponent reactions for facile access to coumarin-fused dihydroquinolines and quinolines: Synthesis and photophysical studies

A simple and straightforward method for facile access to coumarin-fused dihydroquinolines (4) has been developed using the microwave-assisted multicomponent reactions of 4-hydroxycoumarin, aldehydes and aromatic amines in water catalyzed by bismuth triflate. Under solvent-free and conventional heating conditions, the same combination provided the corresponding coumarin-fused quinolines (5). An alternative and rapid method for the conversion of (4) to (5) with very good yields was also developed using N-bromosuccinamide. Single-crystal X-ray crystallographic analysis of one of the products (4q) showed that the products are regioselective and that the reactions proceed via 1,2-addition followed by 6pi-electrocyclization instead of a Skraup-Doebner-von Miller type reaction. Substituted quinoline carboxylic acid derivatives (7) were synthesized selectively from (4) by ring opening of the coumarin moiety followed by aromatization using NaOH/DMSO under reflux conditions. Considering the presence of the polycyclic conjugated structure of the synthesized compounds 4 and 5 with the coumarin moiety, preliminary photophysical studies were carried out and promising quantum yields were observed along with a maximum quantum yield (of = 0.65) for 4j.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Interrupted imino-nazarov cyclization of 1-aminopentadienyl cation and related cascade process

Facile 4pi conrotatory imino-Nazarov cyclization of a 1-aminopentadienyl cation generated from condensation an aldehyde and secondary aniline in the presence of a catalytic amount of a Lewis acid has been developed. Silver(I)-catalyzed intramolecular arene trapping of the resulting cyclic oxyallyl cation leads to formation of tricyclic indoline-fused cyclopentanone. The use of lanthanide salts allows transformation after the initial trapping to afford tetrahydroquinoline-fused cyclopentenone in a concise manner. Taking control: The fate of an oxyallyl cation formed through a 4pi conrotatory imino-Nazarov cyclization can be controlled to access cyclopentanoid frameworks. In the presence of silver(I), intramolecular arene trapping leads to indoline-fused cyclopentanones. Gadolinium(III) facilitates a cascade transformation to furnish tetrahydroquinoline-fused cyclopentenones. Tf=trifluoromethanesulfonyl.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Unexpected Oxidative Ring Opening of Electron-Rich 3-Aminobenzofurans into alpha-Ketoimines Derivatives

An unexpected ring opening of 3-aminobenzofurans promoted by NaOtBu in hot toluene, leading to a variety of alpha-ketoimines, is described. In the presence of 3-iodobenzofurans, NaOtBu mediates the 3-aminobenzofurans ring opening via a possible radical pathway without the help of any external radical sources.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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The structure-activity relationships of A-ring-substituted aromathecin topoisomerase i inhibitors strongly support a camptothecin-like binding mode

Aromathecins are inhibitors of human topoisomerase I (Top1). These compounds are composites of several heteroaromatic systems, namely the camptothecins and indenoisoquinolines, and they possess notable Top1 inhibition and cytotoxicity when substituted at position 14. The SAR of these compounds overlaps with indenoisoquinolines, suggesting that they may intercalate into the Top1-DNA complex similarly. Nonetheless, the proposed binding mode for aromathecins is purely hypothetical, as an X-ray structure is unavailable. In the present communication, we have synthesized eight novel series of A-ring-substituted (positions 1-3) aromathecins, through a simple, modular route, as part of a comprehensive SAR study. Certain groups (such as 2,3-ethylenedioxy) moderately improve Top1 inhibition, and, often, antiproliferative activity, whereas other groups (2,3-dimethoxy and 3-substituents) attenuate bioactivity. Strikingly, these trends are very similar to those previously observed for the A-ring of camptothecins, and this considerable SAR overlap lends further support (in the absence of crystallographic data) to the hypothesis that aromathecins bind in the Top1 cleavage complex as interfacial inhibitors in a ‘camptothecin-like’ pose.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The Absolute Best Science Experiment for 22013-33-8

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PYRAZOLE DERIVATIVES AS P38 MAP INHIBITORS

Compounds of formula (I): wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn’s disease and of the eye, such as uveitis.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Properties and Exciting Facts About 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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 22013-33-8 is helpful to your research. Reference of 22013-33-8

Reference of 22013-33-8, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 22013-33-8, molcular formula is C8H9NO2, introducing its new discovery.

METHODS AND COMPOSITIONS RELATED TO EOSINOPHIL REGULATION

Disclosed are compositions and methods for regulating eosinophils.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2

N,N-bis-heteroaryl methylamines: Potent anti-mitotic and highly cytotoxic agents

The synthesis and evaluation of a series of N,N-bis-heterocyclic-methylamines 1 as isoazaerianin analogues are described. It was demonstrated that the replacement of the 3,4,5-trimethoxyphenyl A-ring present in CA-4, isoCA-4 and isoazaerianin by a quinoline or a quinazoline ring is possible and often beneficiary for a high level of cytotoxicity. We have also showed that a carbazole or an indole nucleus are very effective as B-rings in this series, leading to anti-cancer drugs 1 having a sub-nanomolar level of cytotoxicity (1a: IC50 = 70 pM against HCT116 cells). 1a also display a high level of cytotoxicity against four other human cancer cells and inhibited tubulin assembly at a micromolar level. Moreover, at a concentration of 5 nM, 1a arrested the cellular cycle in G2/M phase of the cellular cycle and induced apoptosis of HCT116 cells. It was also showed that after few hours 1a at a concentration of 10 nM totally disrupted endothelial network formation on Matrigel.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Brief introduction of 22013-33-8

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 22013-33-8. In my other articles, you can also check out more blogs about 22013-33-8

Application of 22013-33-8, 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. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a Article£¬once mentioned of 22013-33-8

Synthesis of tetrahydro-1H,7H-benzo[ij]quinolizine-1,7-dione derivatives

Tetrahydro-1H,7H-benzo[ij]quinolizine-1,7-diones have been obtained by the cyclization of N-alkoxyphenyl-N-(2-carboxyethyl)-beta-alanines. Fission of the ester bond occurs on cyclization of N-(4-ethoxyphenyl)-N-(2-carboxyethyl)-beta-alanine, but the cyclization of the 3,4-dialkoxyphenyl derivative leads to the formation of 9-alkoxy-8-hydroxy-2,3,5,7-tetrahydro-1H,7H-benzo[ij]quinolizine-1,7-diones. The corresponding dioximes and diphenylhydrazones were obtained.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Top Picks: new discover of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Synthesis of 5-amino-1-aryl-4-(4-aryl-1,3-thiazol-2-yl)-2,3-dihydro-1H-pyrrol-3-ones

Reactions of 2-(4-aryl-1,3-thiazol-2-yl)-3-oxo-4-chlorobutyronitriles with primary aromatic amines result in nucleophilic substitution of the chlorine atom by amino group, followed by intramolecular addition of the secondary amino group to the cyano group. The products are 5-amino-1-aryl-4-(4-aryl-1,3-thiazol-2-yl)-2,3-dihydro-1H-pyrrol-3-ones which are structurally related to the known antiischemic drugs.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem