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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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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Direct carboxylation of simple arenes under atmospheric pressure of CO2 is achieved through a rhodium-catalyzed C-H bond activation without the assistance of a directing group. Various arenes such as benzene, toluene, xylene, electron-rich or electron-deficient benzene derivatives, and heteroaromatics are directly carboxylated with high TONs. This journal is

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Benzodioxan,
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A Pd(II)-catalyzed reaction protocol for the direct carboxylation of benzoic and phenylacetic acid derivatives to form dicarboxylic acids has been developed. The reaction conditions are also applicable for the carboxylation of vinyl C-H bonds. The first C-H insertion Pd-aryl complex from carboxylic acids has been characterized by X-ray crystallography. Copyright

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Benzodioxan,
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A carboxylate-directed ortho-C?H functionalization has been developed and it allows the regiospecific introduction of allyl residues to benzoic acids. In the presence of a [Ru(p-cymene)Cl2]2 and K3PO4, benzoic acids react with allyl acetates at only 50 C to give the corresponding ortho-allylbenzoic acids. The protocol is generally applicable to both electron-rich and electron-poor benzoic acids in combination with linear and branched allyl acetates. The products can be further functionalized in situ, for example, by double-bond migration, lactonization, or decarboxylation.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A palladium-catalyzed carboxylic acid-directed cross-coupling of an ortho-C(sp2) atom of aromatic acids with aliphatic aziridines to construct the beta-arylethylamine skeleton via C-H activation has been developed. The reaction proceeded under mild conditions with great substrate scope. Meanwhile, the beta-arylethylamine skeleton in drugs or bioactive compounds could be easily generated in a single step. A catalytic amount of cesium carbonate was crucial to realizing the selective beta-arylethylamine synthesis.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the com­pounds and using the compounds for treatment of dis­eases associated with LRRK2 receptor, such as Parkin­son?s disease

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3, are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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Benzodioxan,
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The invention relates to compound of general formula (I): STR1 wherein: Z represents O or CH 2n is from 0 to 4R, X and Y are as defined in the description, andA represents STR2 wherein R 1, R 2, R 6, R 7 and T” are as defined in the description,and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

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A series of 2-styryl-5-nitroimidazole derivatives containing 1,4-benzodioxan moiety (3a-3r) has been designed, synthesized and their biological activities were also evaluated as potential antiproliferation and focal adhesion kinase (FAK) inhibitors. Among all the compounds, 3p showed the most potent activity in vitro which inhibited the growth of A549 with IC 50 value of 3.11 muM and Hela with IC50 value of 2.54 muM respectively. Compound 3p also exhibited significant FAK inhibitory activity (IC50 = 0.45 muM). Docking simulation was performed for compound 3p into the FAK structure active site to determine the probable binding model.

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Benzodioxan,
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Demonstrating intracellular protein target engagement is an essential step in the development and progression of new chemical probes and potential small molecule therapeutics. However, this can be particularly challenging for poorly studied and noncatalytic proteins, as robust proximal biomarkers are rarely known. To confirm that our recently discovered chemical probe 1 (CCT251236) binds the putative transcription factor regulator pirin in living cells, we developed a heterobifunctional protein degradation probe. Focusing on linker design and physicochemical properties, we generated a highly active probe 16 (CCT367766) in only three iterations, validating our efficient strategy for degradation probe design against nonvalidated protein targets.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem