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Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors

It had been reported that some dioxygenated rings fusing with the quinazoline scaffold could lead to new EGFR inhibitors. Based on this, several kinds of oxygenated alkane quinazoline derivatives were synthetized and evaluated as EGFR inhibitors. Their antiproliferative activities were tested against four cancer cell lines: A431, MCF-7, A549, and B16-F10. Most derivatives could counteract EGF-induced EGFR phosphorylation, and their potency was comparable to the reference compound Erlotinib. The size of the fused dioxygenated ring was crucial for the biological activity and the heptatomic ring derivative 19 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the cellular assay.

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

Simple exploration of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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Solution phase synthesis of a spiro[pyrrolidine-2,3′-oxindole] library via a three component 1,3-dipolar cycloaddition reaction

A combinatorial library of 26,500 spiro[pyrrolidine,-2,3-oxindoles] was prepared in a single-compound format by a facile intermolecular 1,3-dipolar cycloaddition. An azomethine ylide, generated by the decarboxylative condensation of an isatin 1 with an alpha-amino acid 2, was trapped by a transchalcone 3 to afford heterocycles of the general structure 4. The regio- and stereochemistry of a representative product was determined by single crystal X-ray structure.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

A new application about 10288-72-9

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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, 10288-72-9, molcular formula is C8H8O3, introducing its new discovery. 10288-72-9

Substituted heterocyclic compounds, method for preparing and compositions containing same

The invention relates to compounds of formula (I): wherein:R1, R2 and R3 are as defined in the description,X is as defined in the description,Y represents an oxygen atom, a sulphur atom, a C(H)q group, SO or SO2,n is equal to from 0 to 5,A represents a NR5R6 group,and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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2879-20-1, An article , which mentions 2879-20-1, molecular formula is C10H10O3. The compound – 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone played an important role in people’s production and life.

Studies of arylthiazole oxamates in relation to oral antiallergic activity

25 arylthiazole oxamate derivatives were synthesized and examined for antiallergic activity in the rat passive cutaneous anaphylaxis assay. These compounds were prepared by treatment of the appropriate bromoacetophenone with thioureas to give arylaminothiazoles. Further condensation with alkyloxalyl chloride gave the arylthiazolyl oxamates. Several derivatives showed a 70% inhibition at 5 mg/kg p.o. p-Alkoxy substitution on the phenyl ring resulted in enhanced activity while N-alkyl substitution on the nitrogen amide function inhibited the activity. Ethyl-N-(4-p-methoxyphenyl)-2-thiazolyl oxamate (tioxamast, F-1865) was selected for clinical studies.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS

Pyrimidine ethers and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 22013-33-8, C8H9NO2. A document type is Article, introducing its new discovery., 22013-33-8

Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors

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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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about (S)-1,4-Benzodioxane-2-carboxylic acid

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Because a catalyst decreases the height of the energy barrier, 70918-54-6, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, molecular formula is C9H8O4. In a article£¬once mentioned of 70918-54-6

Synthesis and cytotoxic activities of a series of novel N -methyl-bisindolylmaleimide amide derivatives

A novel series of N-methyl-bisindolylmaleimides were synthesized and evaluated for their inhibitory activities against nine tumor cell lines. Some of the compounds showed an interesting activity against the tested cell lines. The most potent compounds 5e and 5j displayed antiproliferative activity with 50% inhibitory concentration values in the muM range against some tested cell lines.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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2879-20-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone,introducing its new discovery.

Ruthenium Complexes Immobilized on Functionalized Knitted Hypercrosslinked Polymers as Efficient and Recyclable Catalysts for Organic Transformations

A hypercrosslinked polymer (HCP)-immobilized ruthenium catalyst (HCP?PPh3?Ru) was prepared from benzene and triphenylphosphine (PPh3) through a one-step external cross-linking reaction. The structure and composition of the catalyst were fully characterized by many physicochemical methods. HCP?PPh3?Ru was found to possess high Brunauer?Emmett?Teller (BET) surface area, large pore volume, and low skeletal density. Moreover, the Ru catalyst was also featured some advantages, such as low synthetic cost and good chemical and thermal stability. HCP?PPh3?Ru was then used as a recoverable and effective catalyst for the synthesis of 2,4-diaryl-substituted pyridines from acetophenones, ammonium acetate (NH4OAc) and dimethylformamide (DMF), and the cycloaddition reaction of diazodicarbonyl compounds with olefins to afford dihydrofurans. In addition, a combination of HCP?PPh3?Ru and Amberlyst-15 enabled us to establish a simple protocol for the direct synthesis of carbazole derivatives from diazodicarbonyl compound, alkyl vinyl ether and indole. In these selected reactions, the catalyst was easily recovered and reused several times without significant activity loss. (Figure presented.).

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

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Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor beta-selective agonists

A novel series of 1,3-bistrifluoromethylcarbinol derivatives that act as liver X receptor (LXR) beta-selective agonists was discovered. Structure-activity relationship studies led to the identification of molecule 62, which was more effective (Emax) and selective toward LXRbeta than T0901317 and GW3965. Furthermore, 62 decreased LDL-C without elevating the plasma TG level and significantly suppressed the lipid-accumulation area in the aortic arch in a Bio F1B hamster fed a diet high in fat and cholesterol. We demonstrated that our LXRbeta agonist would be potentially useful as a hypolipidemic and anti-atherosclerotic agent. In this manuscript, we report the design, synthesis and pharmacology of 1,3-bistrifluoromethylcarbinol derivatives.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of (S)-1,4-Benzodioxane-2-carboxylic acid

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4-PIPERAZINNYLTHIENO [2,3-D] PYRIMIDINE COMPOUNDS AS PLATELET AGGREGATION INHIBITORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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