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

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Reference of 4442-53-9, Chemical Research Letters, May 2021.In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,introducing its new discovery.

Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.

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

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Achiral pyran-2-one analogs possessing a 3-S-(2-alkylphenyl) group were determined to be high-affinity inhibitors for human immunodeficiency virus (HIV) protease (PR). Crystallographic, modeling, and structure-activity studies led to the 3-S-(2-tert-butylphenyl) moiety as an apparent optimal group to access the S2?/S1? pockets of the enzyme. Further optimization led to an inhibitor, 3-[(2-tert-butylphenyl)sulfanyl]-4-hydroxy-6-(3-methylphenyl)-pyran-2-one (14), possessing a Ki of 3 nM. An X-ray crystallographic structure of an inhibitor, 4-hydroxy-3-[(2-isopropylphenyl)sulfanyl]-6-phenylpyran-2-one (8), bound to HIV PR showed that the 3-S-(2-isopropylphenyl) group occupied the P2? and P1? pockets, while other crucial interactions were common to those found with other pyran-2-one analogs. The high potency observed for this series may be due, in part, to the restrictions on the intramolecular collapsibility of these molecules in aqueous solution, leading to a highly favorable hydrophobic effect on binding. Herein we report a novel P2?/P1? achiral ligand which results in a tight-binding inhibitor that occupies only three pockets in the enzyme and exhibits a unique pattern of in vitro resistance.

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

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One of the oldest and most widely used commercial enzyme inhibitors is aspirin, HPLC of Formula: C9H8O4, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 70918-54-6

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Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.

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

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A copper-catalyzed 8-amide chelation-assisted C-H alkylation of 8-aminoquinolines is described. The secondary and tertiary alkyl carboxylic acids can be used as alkylating agents. This reaction allows for the highly regioselective preparation of C2-adamantyl 8-aminoquinoline scaffolds by the decarboxylative alkylation catalytic system.

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

A new application about C8H9NO2

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Photoswitches capable of accessing two geometric states are highly desirable, especially if their design is modular and incorporates a pharmacophore tethering site. We describe a redox isomerization strategy for synthesizing p-formylazobenzenes from p-nitrobenzyl alcohol. The resulting azo-aldehydes can be readily converted to photoswitchable compounds with excellent photophysical properties using simple hydrazide click chemistry. As a proof of principle, we synthesized a photoswitchable surfactant enabling the photocontrol of an emulsion with exceptionally high spatiotemporal precision.

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

Brief introduction of C8H9NO2

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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. Quality Control 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

High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.

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

Archives for Chemistry Experiments of C8H9NO2

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

Chemical Research Letters, May 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. Which mentioned a new discovery about Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

Highly selective reduction of nitroarenes has been achieved using iron metal nanoparticles in water at room temperature. A wide spectrum of reducible functionalities remained inert under the reaction conditions. During the reaction a change in shape of Fe nanoparticles was observed.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

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

Archives for Chemistry Experiments of C10H10O3

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A new one-pot palladium-catalyzed process between N-tosylhydrazones, N-(dihalophenyl)-imidates, and amines was designed. This reaction involves Barluenga cross-coupling and N-arylation followed by cyclization to produce functionalized benzimidazoles. During this transformation, one C=C bond and two C=N bonds were created by a single palladium-catalyzed reaction. Depending on the starting materials, a library of 5-(1-arylvinyl)-1H-benzimidazoles was synthesized. Among several arylvinylbenzimidazole derivatives evaluated, one compound exhibits excellent antiproliferative activity in the nanomolar concentration range against human colon carcinoma cell lines (HCT-116) and human lung adenocarcinoma epithelial cell lines (A549).

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

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Studies on the discovery of tyrosinase enzyme inhibitors and exploration for better cytotoxic agents remain an important line in drug discovery and development. A series of synthetic chalcones and pyrazoline derivatives was evaluated for their inhibitory effects on the diphenolase activity of mushroom tyrosinase. The effects of these compounds on proliferation and microtubule assembly were also evaluated in seven different cancer cell lines. The results revealed that some of the synthetic compounds showed significant inhibitory activity, with four compounds being more potent tyrosinase inhibitors than the reference standard inhibitor kojic acid. Several compounds were toxic to cancer cell lines. Compound 1a was found to possess the highest anticancer activity towards all cell lines with an IC50 in the range of 0.9-2.2 muM. Seven of the compounds showed considerable tubulin polymerization activity at a concentration of 25 muM. Molecular modeling studies of these synthetic compounds were performed to investigate their interactions with the tyrosinase enzyme. The structure-activity relationship (SAR) study using in-silico analysis matched well with the in vitro tumour cell inhibitory activity.

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