Archives for Chemistry Experiments of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core

A series of simplified ring-opened resorcylic acid lactone (RAL) derivatives were conveniently synthesized to target FLT3 and its mutants either irreversibly or reversibly. Our design of covalent FLT3 inhibitors is based on cis-enone RALs (e.g., L-783,277) that have a beta-resorcylic acid as the core structure. The designed compounds contain three types of Michael acceptors (acrylamide, vinylsulfonamide and maleimide) as potential covalent traps of a cysteine residue at the binding site of kinases. A variety of functional substitutions were also introduced to maximize the binding interactions. Biological evaluations revealed that compound 17, despite the presence of a highly reactive maleimide Michael acceptor, is a potent covalent FLT3 inhibitor which shows some specificity in cellular assays. On the other hand, compounds 2 and 6 containing acrylamide or vinylsulfonamide groups are reversible towards FLT3 binding, and are potent and selective inhibitors of mutant FLT3-ITD versus wt-FLT3. They also inhibit cell proliferation in FLT3-ITD expressing cell line MV-4-11 as compared to wt-FLT3 expressing cell line THP-1 and non-FLT3 cell lines (K562, HL60 and Hek-293T).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome Chemistry Experiments For 22013-33-8

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A benzo heterocyclic structure containing organic photoelectric material and its preparation method and application (by machine translation)

The invention belongs to the photoelectric material applied science and technology field, in particular to a benzo heterocyclic structure containing organic photoelectric material and its application. At the same time the material is in the west of five-membered imidazole nitrogen atom site is introduced on the polycyclic aromatic hydrocarbon and carbon atom site is introduced on the […] heterocyclic, a single or three heavy condition can the crack at the same time meet the Delta EST The triplet energy level is relatively small and the receptor of the excited state of the two times higher than the single material, RISC and TTA coexistence system electroluminescent mechanism in order to obtain high photoelectric conversion efficiency and the solves the dark blue light material efficiency […] and light color and quality problems and provides a practical way. For/receptor through the choice and the design of the structure, the present invention provides benzo heterocyclic structure containing organic photoelectric material independent as luminescent material or as a doping material in the luminescent layer in the organic electroluminescent device are performance excellent performance, synthesis and purification process is simple, can be suitable for industrial production. (by machine translation)

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome and Easy Science Experiments about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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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. Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acidIn an article, once mentioned the new application about 4442-53-9.

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological results for these compounds indicate on average a lower clogP limit of about 5.0 in this series for retention of potent inhibitory activity (MIC90s) against M.tb in culture. Some of the compounds also showed a significant reduction in inhibition of hERG channel potassium current compared with bedaquiline, but there was no common structural feature that distinguished these.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extended knowledge of 22013-33-8

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Synthetic Route of 22013-33-8, 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, 22013-33-8, molcular formula is C8H9NO2, introducing its new discovery.

Photoredox-Catalyzed Four-Component Reaction for the Synthesis of Complex Secondary Amines

The one-pot sulfonylation/aminoalkylation of styrene derivatives furnishing substituted I3-sulfonylamines was accomplished through a photoredox-catalyzed four-component reaction. Besides one molecule of water and the sodium counterion of the sulfinate, all atoms of the starting materials are transferred to the final product, rendering this process highly atom-efficient. The operationally simple protocol allows for the simultaneous formation of three new single bonds (C-S, C-N, and C-C) and therefore grants rapid access to structurally diverse products.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about 214894-89-0

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2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1- yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability

In this paper we describe the synthesis of a series of alpha-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1’S,2’S)-carboxycyclopropylglycine (2, L-CCG 1). Incorporation of a substituent on the amino acid carbon converted the agonist 2 into an antagonist. All of the compounds were prepared and tested as a series of four isomers, i.e., two racemic diastereomers. On the basis of the improvement in affinity realized for the alpha-phenylethyl analogue 3, in this paper we explored the effects of substitution on the aromatic ring as a strategy to increase the affinity of these compounds for group II mGluRs. Affinity for group II mGluRs was measured using [3H]glutamic acid (Glu) binding in rat forebrain membranes. Antagonist activity was confirmed for these compounds by measuring their ability to antagonize (1S,3R)-1- aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells transfected with human mGluR2 and mGluR3. Meta substitution on the aromatic ring of 3 with a variety of substituents, both electron donating (e.g., methyl, hydroxy, amino, methoxy, phenyl, phenoxy) and electron withdrawing (e.g., fluorine, chlorine, bromine, carboxy, trifluoromethyl) gave from 1.5- to 4.5-fold increases in affinity. Substitution with p-fluorine, as in 97 (IC50 = 0.022 ¡À 0.002), was the exception. Here, a greater increase in affinity was realized than for either the ortho- or meta-substituted analogues; 97 was the most potent compound resulting from monosubstitution of the aromatic. At best, only modest increases in affinity were realized for certain compounds bearing either two chlorines or two fluorines, and two methoxy groups gave no improvement in affinity (all examined in a variety of substitution patterns). Three amino acids, 4, 5, and 104, were resolved into their four constituent isomers, and affinity and functional activity for group II mGluRs was found to reside solely in the S,S,S-isomers of each, consistent with 1. With an IC50 = 2.9 ¡À 0.6 nM, the resolved xanthylmethyl compound 168 was the most potent compound from this SAR. Amino acid 168 demonstrated high plasma levels following intraperitoneal (ip) administration and readily penetrated into the brain. This compound, however, had only limited (~5%) oral bioavailability. Systemic administration of 168 protected mice from limbic seizures produced by the mGluR agonist 3,5-dihydroxyphenylglycine, with an ED50 = 31 mg/kg (ip, 60 min preinjection). Thus, 168 represents a valuable tool to study the role of group II mGluRs in disease.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Top Picks: new discover of 2879-20-1

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Reference of 2879-20-1, 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, 2879-20-1, molcular formula is C10H10O3, introducing its new discovery.

A new protocol for the construction of pyrrolo[4,3,2-de]quinolinones

A facile method has been suggested for constructing pyrrolo[4,3,2-de]quinolinones by addition of acetophenones to 4-nitroisatin followed by reduction of the nitro group and spontaneous cyclisation.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New explortion of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them

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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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for (S)-1,4-Benzodioxane-2-carboxylic acid

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Direct synthesis of N-acylalkylenediamines from carboxylic acids under mild conditions

Monoacylated piperazine derivatives were prepared directly from carboxylic acids and piperazine using triphenylphosphine (TPP) and N-bromosuccinimide (NBS) in dichloromethane. Inexpensive and readily available reagents, excellent yields, short reaction times and mild reaction conditions are important features of this method.

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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

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Discovery of novel aminothiadiazole amides as selective EP3 receptor antagonists

This Letter discloses a series of 2-aminothiadiazole amides as selective EP3 receptor antagonists. SAR optimization resulted in compounds with excellent functional activity in vitro. In addition, efforts to optimize DMPK properties in the rat are discussed. These efforts have resulted in the identification of potent, selective EP3 receptor antagonists with excellent DMPK properties suitable for in vivo studies.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. HPLC of Formula: C9H9BrO2. Introducing a new discovery about 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use

The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

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