The Absolute Best Science Experiment for 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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3,3-DIFLUORO-PIPERIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS

Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).

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

Some scientific research about 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Quality Control of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 214894-89-0, name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine. In an article£¬Which mentioned a new discovery about 214894-89-0

Novel carbamate derivatives of 4-beta-amino-4?-O-demethyl-4- desoxypodophyllotoxin as inhibitors of topoisomerase II: Synthesis and biological evaluation

A novel series of carbamate derivatives of 4-beta-amino-4?-O- demethyl-4-desoxypodophyllotoxin were synthesized. Their effect on human DNA topoisomerase II and antiproliferative activity was evaluated. Compounds 4a-c, 4g, 4j and 4k are topoisomerase II poisons that induce double-stranded breaks in DNA and exhibit increased cytotoxicity compared to etoposide. The Royal Society of Chemistry 2005.

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

Top Picks: new discover of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Effect of O6-substituted guanine analogs on O6-methylguanine DNA-methyltransferase Expression and glioblastoma cells viability

Background: Glioblastoma multiforme (GBM) is often associated with a poor survival prognostic for patients. The main reason seems to be the acquired or inherent resistance to the chemotherapeutic agent used to treat the tumor, temozolomide (TMZ). To this day, the most recognized pathway of resistance is the DNA Direct Repair pathway by the means of the protein O6-methylguanine DNA-methyltransferase (MGMT). Objectives: To design and synthesize a series of MGMT inhibitors that can sensitize GBM cells to TMZ. Methods: Twenty-five O6-alkyl, O6-aryl and O6-substituted-aryl guanine analogs including nine novel compounds were synthesized, characterized, analyzed by molecular docking and tested on the T98G GBM cells viability. Results: Following molecular modeling with MGMT, the newly designed compounds 19, 22, and 24 emerged as the most promising MGMT ligands and displayed modest cytotoxicity. Guanine analog (19), bearing a p-nitrobenzyl moiety, reduced considerably the O6-methylguanine DNA-methyltransferase expression level. When combined with TMZ (1), which is used as first line treatment for brain tumors, compounds 19, 22, and 24 decreased T98G cellsoproliferation by 32%, 68% and 50%, respectively. TMZ (1) displayed negligible effect on the proliferation of these cells further supporting the notion that this cell model is resistant to this alkylating agent. Conclusion: Overall, these results notably highlight a group of MGMT inhibitors that warrants further exploration in the development of therapeutic options to circumvent TMZ resistance in brain tumors.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Top Picks: new discover of 214894-89-0

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CuBr2 catalyzed bromination/oxidation of isochromans to benzaldehyde derivatives

A series of isochromans were oxidized and brominated by using 1.2 equiv of CuBr2 in CH3CN at reflux to give the corresponding bromo benzaldehydes in moderate yields. A plausible mechanism for this transformation has been suggested.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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C -Methylation of Alcohols, Ketones, and Indoles with Methanol Using Heterogeneous Platinum Catalysts

A versatile, selective, and recyclable heterogeneous catalytic method for the methylation of C-H bonds in alcohols, ketones, and indoles with methanol under oxidant-free conditions using a Pt-loaded carbon (Pt/C) catalyst in the presence of NaOH is reported. This catalytic system is effective for various methylation reactions: (1) the beta-methylation of primary alcohols, including aryl, aliphatic, and heterocyclic alcohols, (2) the alpha-methylation of ketones, and (3) the selective C3-methylation of indoles. The reactions are driven by a borrowing-hydrogen mechanism. The reaction begins with the dehydrogenation of the alcohol(s) to afford aldehydes, which subsequently undergo a condensation reaction with the nucleophile (aldehyde, ketone, or indole), followed by hydrogenation of the condensation product by Pt-H species to yield the desired product. In all of the methylation reactions explored in this study, the Pt/C catalyst exhibits a significantly higher turnover number than other previously reported homogeneous catalytic systems. Moreover, it is demonstrated that the high catalytic activity of Pt can be rationalized in terms of the adsorption energy of hydrogen on the metal surface, as revealed by density functional theory calculations on different metal surfaces.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Synthesis, Antiplatelet Aggregation Activity Evaluation and 3D-QSAR of a Series of Novel 6-Alkylamino(Alkoxyl)-2-Propylthio-8-Azapurine Nucleosides

A series of novel 6-alkylamino(alkoxyl)-2-propylthio-8-azapurine nucleosides were synthesized by an improved route, and the human antiplatelet aggregation activities of these new compounds were evaluated. A self-organizing molecular field analysis method was used to study the three-dimensional quantitative structure?activity relationship of these novel nucleosides. The results of the antiplatelet aggregation activity evaluation and analysis of the self-organizing molecular field analysis models through shape and electrostatic grids may provide a basis for the development of new and potent antiplatelet agents.

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

Discovery of 214894-89-0

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214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, belongs to benzodioxans compound, is a common compound. COA of Formula: C9H9BrO2In an article, once mentioned the new application about 214894-89-0.

Selective synthesis of substituted benzylic alcohols from aromatic substrates included in beta-cyclodextrin

The regio- and enantioselective reduction of substituted styrenic epoxides and aromatic ketones by borohydride in the presence of beta-cyclodextrin is described. The regioselectivity is related to the hydrophobicity of the substrate, which governs its penetration inside the cavity of the cyclodextrin and is favorable to the beta-opening of the epoxide. The stereoselectivity observed during the reduction is mainly dependent on the non-covalent interactions between the upper rim of the cyclodextrin and the substrate included in it. The chimioselectivity observed during the reduction of ketoester is assumed to be dependent on an alkoxyborohydride intermediate formed in the first step of the reaction. Elsevier.

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

Extracurricular laboratory:new discovery of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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New substituted isochromans

Isochromans with substituents in the aromatic ring are described. They are synthesised by cyclisation of related chloromethyl-2-phenylethyl ethers. The activated 1-position of the isochromans is essential for obtaining potential drugs.

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

Some scientific research about 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Novel Hypoxia-Inducible Factor 1alpha (HIF-1alpha) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy

Ocular diseases featuring pathologic neovascularization are the leading cause of blindness, and anti-VEGF agents have been conventionally used to treat these diseases. Recently, regulating factors upstream of VEGF, such as HIF-1alpha, have emerged as a desirable therapeutic approach because the use of anti-VEGF agents is currently being reconsidered due to the VEGF action as a trophic factor. Here, we report a novel scaffold discovered through the complete structure-activity relationship of ring-truncated deguelin analogs in HIF-1alpha inhibition. Interestingly, analog 6i possessing a 2-fluorobenzene moiety instead of a dimethoxybenzene moiety exhibited excellent HIF-1alpha inhibitory activity, with an IC50 value of 100 nM. In particular, the further ring-truncated analog 34f, which showed enhanced HIF-1alpha inhibitory activity compared to analog 2 previously reported by us, inhibited in vitro angiogenesis and effectively suppressed hypoxia-mediated retinal neovascularization. Importantly, the heteroatom-substituted benzene ring as a key structural feature of analog 34f was identified as a novel scaffold for HIF-1alpha inhibitors that can be used in lieu of a chromene ring.

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

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Simplified 2-aminoquinoline-based scaffold for potent and selective neuronal nitric oxide synthase inhibition

Since high levels of nitric oxide (NO) are implicated in neurodegenerative disorders, inhibition of the neuronal isoform of nitric oxide synthase (nNOS) and reduction of NO levels are therapeutically desirable. Nonetheless, many nNOS inhibitors mimic l-arginine and are poorly bioavailable. 2-Aminoquinoline-based scaffolds were designed with the hope that they could (a) mimic aminopyridines as potent, isoform-selective arginine isosteres and (b) possess chemical properties more conducive to oral bioavailability and CNS penetration. A series of these compounds was synthesized and assayed against purified nNOS enzymes, endothelial NOS (eNOS), and inducible NOS (iNOS). Several compounds built on a 7-substituted 2-aminoquinoline core are potent and isoform-selective; X-ray crystallography indicates that aminoquinolines exert inhibitory effects by mimicking substrate interactions with the conserved active site glutamate residue. The most potent and selective compounds, 7 and 15, were tested in a Caco-2 assay and showed good permeability and low efflux, suggesting high potential for oral bioavailability.

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