Archives for Chemistry Experiments of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

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

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Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease

Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic effects, it has been suggested that the CB1 receptors in the periphery could play a significant role in reducing reflux. A moderately potent and highly lipophilic series of 2-aminobenzamides was identified through focused screening of GPCR libraries. Development of this series focused on improving potency and efficacy at the CB1 receptor, reducing lipophilicity and limiting the central nervous system (CNS) exposure while maintaining good oral absorption. Improvement of the series led to compounds having excellent potency at the CB1 receptor and high levels of agonism, good physical and pharmacokinetic properties, and low penetration into the CNS. A range of compounds demonstrated a dose-dependent inhibition of transient lower esophageal sphincter relaxations in a dog model.

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

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Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-beta type 1 receptor inhibitors

Inhibition of transforming growth factor beta (TGF-beta) type 1 receptor (ALK5) provides a feasible approach for the treatment of fibrotic diseases and malignant tumors. In this study, we designed and synthesized a new series of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives, and evaluated biologically as TGF-beta type 1 receptor inhibitors. The most potent compound 15r inhibited the ALK5 enzyme and NIH3T3 cell viability with IC50 values of 44 and 42.5 nM, respectively. Compound 15r also displayed better oral plasma exposure and excellent bioavailability than LY-3200882, and in vivo inhibited 65.7% of the tumor growth in a CT26 xenograft mouse model.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Direct carboxylation of simple arenes with CO2 through a rhodium-catalyzed C-H bond activation

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,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis, biological evaluation, and molecular docking studies of novel 2-styryl-5-nitroimidazole derivatives containing 1,4-benzodioxan moiety as FAK inhibitors with anticancer activity

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

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3-AZA-BICYCLO[3.3.0]OCTANE COMPOUNDS

The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 4442-53-9, and how the biochemistry of the body works.Electric Literature of 4442-53-9

Electric Literature of 4442-53-9, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,introducing its new discovery.

Discovery of cell-permeable inhibitors that target the BRCT domain of BRCA1 protein by using a small-molecule microarray

BRCTs are phosphoserine-binding domains found in proteins involved in DNA repair, DNA damage response and cell cycle regulation. BRCA1 is a BRCT domain-containing, tumor-suppressing protein expressed in the cells of breast and other human tissues. Mutations in BRCA1 have been found in ca. 50% of hereditary breast cancers. Cell-permeable, small-molecule BRCA1 inhibitors are promising anticancer agents, but are not available currently. Herein, with the assist of microarray-based platforms, we have discovered the first cell-permeable protein-protein interaction (PPI) inhibitors against BRCA1. By targeting the (BRCT)2 domain, we showed compound 15a and its prodrug 15b inhibited BRCA1 activities in tumor cells, sensitized these cells to ionizing radiation-induced apoptosis, and showed synergistic inhibitory effect when used in combination with Olaparib (a small-molecule inhibitor of poly-ADP-ribose polymerase) and Etoposide (a small-molecule inhibitor of topoisomerase II). Unlike previously reported peptide-based PPI inhibitors of BRCA1, our compounds are small-molecule-like and could be directly administered to tumor cells, thus making them useful for future studies of BRCA1/PARP-related pathways in DNA damage and repair response, and in cancer therapy.

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

Final Thoughts on Chemistry for 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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Synthesis of 7-substituted-(2,3-dihydro-1,4-benzodioxin-5-yl)-piperazine

A simple and versatile method for the synthesis of 7-substituted (2,3-dihydro-1,4-benzodioxin-5-yl)-piperazines starting from easy available class of derivatives has been developed. Copyright Taylor & Francis Group, LLC.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, belongs to benzodioxans compound, is a common compound. name: 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acidIn an article, once mentioned the new application about 4442-53-9.

Synthesis and phosphodiesterase 5 inhibitory activity of novel phenyl ring modified sildenafil analogues

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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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Application of 4442-53-9, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4. In a article£¬once mentioned of 4442-53-9

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