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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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Four new organic photosensitizers (SH-11?14) that introduced methoxy groups as an additional donor were synthesized, and used in dye-sensitized solar cells. The dyes were designed in order to investigate the effects on the dye photophysical properties and the cell photovoltaic performance, by the number, position, and shape of methoxy groups introduced at the para-/ortho- and para-/meta- and para-(open or closed ring shape) positions on the triphenylamine donor. The introduction of methoxy groups led to bathochromic shift of the absorption spectrum, and enhancement of the molar extinction coefficient of the dyes. Their introduction decreased the amount of dye adsorbed on TiO2surface, due to the increased steric hindrance. As their number increased, an open-circuit voltage value decreased. All things considered, the dye (SH-14) with closed ring shape shows the best conversion efficiency of 6.01% under AM 1.5G conditions (N719 dye’s 7.59% under the same conditions).

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

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Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3- diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

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

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A convenient procedure for the synthesis of quinoxalines and pyridopyrazines has been developed from aryldiamines. The condensation of aminocarbamates such as 12 with ethyl 2,3-dibromopropionate provide the quinoxaline 14 directly, in a one-step operation. The methodology reported herein represents an alternative to condensation of o-phenylenediamines with alpha-dicarbonyl compounds for the quinoxalines formation. The same procedure was applied to the 2,3-diaminopyridine to obtain the corresponding pyridopyrazines.

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

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Application of 22013-33-8, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine,introducing its new discovery.

The present invention relates to novel inhibitors of protein kinase C epsilon (PKCepsilon) signaling, including in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these inhibitors, and their use in the treatment or prevention of disorders such as, e.g., a cardiovascular disorder, cardiac hypertrophy, heart failure, anxiety, pain, chronic pain, migraine, an allergy, an inflammatory disorder, an autoimmune disorder, diabetes, diabetic complications, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic neuropathy, cancer, metastatic cancer, drug-resistant cancer, stomach cancer, lung cancer, thyroid cancer, colon cancer, breast cancer, a neurological disorder, Alzheimer’s disease, Parkinson’s disease, bipolar disorder, stroke, alopecia, or alcoholism.

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

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

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A compound of the formula 1wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.

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

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Application of 22013-33-8, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine,introducing its new discovery.

A new series of 3,4-dihydro-2H-1,3-oxazine derivatives of bakuchiol 1 was synthesized through the Mannich-type condensation-cyclization reaction of 1 with formaldehyde and appropriate primary amines. On cytotoxicity evaluation against a panel of four human cancer cell lines, most of the derivatives showed a higher cytotoxic profile than the parent molecule. The best results were observed for compound 15 with IC50 values of 2, 2, 2.4 and 3 muM against MIA-Pa-Ca-2, HCT-116, MCF-7 and HL-60 cells, respectively. A mechanistic study of compound 15 revealed that it caused a loss in the mitochondrial membrane potential in a concentration-dependent manner, accompanied by the activation of caspase-9 and -3, which cleave PARP-1. It also activated caspase-8, which is involved in the extrinsic apoptotic pathway. Therefore, we demonstrated that it induces apoptosis via both intrinsic and extrinsic pathways in human pancreatic cancer MIA-Pa-Ca-2 cells.

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

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New research progress on 22013-33-8 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Safety of 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 3,1-benzoxazinones, 3,1-benzothiazinones and 4-alkoxyquinazolines have been synthesized via N-aryl-1,2,3-dithiazoles derivatives. The antibacterial and antifungal activity of these compounds were measured; the dithiazoles are significantly active against fungi.

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