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Protein tyrosine phosphatases (PTPs) are potential therapeutic targets for many diseases. Unfortunately, despite considerable drug discovery efforts devoted to PTPs, obtaining selective and cell permeable PTP inhibitors remains highly challenging. We describe a strategy to explore the existing drug space for previously unknown PTP inhibitory activities. This led to the discovery of cefsulodin as an inhibitor of SHP2, an oncogenic phosphatase in the PTP family. Crystal structure analysis of SHP2 interaction with cefsulodin identified sulfophenyl acetic amide (SPAA) as a novel phosphotyrosine (pTyr) mimetic. A structure-guided and SPAA fragment-based focused library approach produced several potent and selective SHP2 inhibitors. Notably, these inhibitors blocked SHP2-mediated signaling events and proliferation in several cancer cell lines. Thus, SPAA may serve as a new platform for developing chemical probes for other PTPs.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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New sildenafil analogues containing an ether ring fused into the phenyl moiety, 6a-d and 7a-d, were efficiently synthesized from the readily available starting materials, 1a-d and 2, in five steps. Ab initio calculations indicated that introduction of a cyclic ether to the phenyl group might enhance the co-planarity of the molecule. The torsional angles were calculated to be 2-3 for the 5-membered cyclic ether derivatives, 6a, 6c, 7a, and 7c, and 12-16 for the 6-membered ones, 6b, 6d, 7b, and 7d. On the other hand, sildenafil showed the least co-planarity with the torsional angle of 23 compared with the target compounds, 6a-d and 7a-d. in the enzyme assay, however, the in vitro PDE 5 inhibitory activity was found out to be inversely related to the degree of co-planarity. In other words, the least planar sildenafil showed the highest actiivty, and the most planar 5-membered cyclic ether derivatives were least active by 100-200-fold compared with sildenafil. Our study clearly demonstrated that the open chain 2′-alkoxy group of the phenyl ring, although less effective for inducing the co-planarity, seemed to act as a much better lipophilic requirement than the cyclic alkoxy moiety. Copyright

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In a patent, 31127-39-6, name is 2,3-Dihydrobenzo[b][1,4]dioxine-6-carbaldehyde oxime, introducing its new discovery. category: benzodioxans

An efficient catalytic method for the synthesis of benzyl- and dibenzylamines by hydrogenating oximes and Schiffbases was developed on palladium supported high-porosity foamed ceramic block catalyst. The multiple regeneration ability of the foamed ceramic block catalyst can significantly decrease the Pd consumption as compared to the use of the conventional 10%Pd/C catalyst. Owing to a high hardness of the foamed ceramic catalyst, the reaction mixture can rapidly be removed from the reactor without using filtering devices. The structures produced by the reaction are fragments of biologically active and natural molecules. Antiproliferative properties of dibenzylamines revealed on the sea urchin embryo model suggest that these compounds can be considered as promising agents for the design of new anticancer drugs.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Research speed reading in 2021.The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. name: 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, 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

Novel benzothiazole derivatives have been synthesised via the corresponding imino-1,2,3-dithiazoles. The cytotoxicity of some of these polyheterocyclic compounds was studied. Our results show that 2-cyano derivatives exhibit a medium in vitro antitumour activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The present invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt, thereof, which may be better selective Wee1 as a new generation, selective inhibitor Wee1 with respect to the existing, inhibitor Wee1 for, Kinase more safe and higher treatment index, and thus has better safety and broader application range, for treatment, of various tumors including brain tumors. (by machine translation)

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Propynyl benzyl ethers having juvenile hormone-like activity which are 4-halogen, lower alkyl, lower alkoxy or propynyloxy substituted or 3,4-lower alkylenedioxy substituted and which can also be 3,5- and/or alpha-substituted, and insecticide compositions that include at least one propynyl benzyl ether and that can also include a conventional insect-poison.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Various new compounds of thiourea were synthesised by reaction of aromatic isothiocyanates with aminoesters. The 1H-NMR and IR spectra were interpreted.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A novel protocol for the synthesis of quinoxalines has been developed from simple ketones and 1,2-diamines. This process underwent a logic approach to bis-substituted quinoxalines via a consecutive iodination/Kornblum oxidation/cyclization in the presence of I2/CuO/DMSO and to mono-substituted quinoxalines via an iodination/cyclization/aromatization in the presence of I2/CuO/K3PO4·3H 2O.

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Benzodioxan,
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Research speed reading in 2021.The prevalence of solvent effects has motivated developing quantitative kinetic, spectroscopic, and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states. Application In Synthesis of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, In a article, mentioned the application of 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, molecular formula is C9H9BrO2

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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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem