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Two series of nitrogenous heterocycle compounds-1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles have been synthesized and evaluated for their ALK5 inhibitory activity and cytotoxicity in TGFbeta-Smad2 assay and MTT assay, respectively. The ALK4/5/7 inhibitory activity of some compound was also evaluated in ALK4/5/7 autophosphorylation assays. Compounds 6c and 14c showed relatively potent ALK5 inhibition while weak cytotoxicity. At the same time, compounds 6c and 14c display relatively better ALK5 selectivity versus ALK4/ALK7 (nearly 10-fold) compared with SB431542, a well known ALK5 inhibitor. Compound 6g2 proved to be a moderately selective ALK4 inhibitor versus ALK5 and ALK7 (>10-fold). The binding mode of 14c generated by flexible docking study shows that 14c fits well into the site cavity of ALK5 by forming several tight interactions.

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

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The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about 22013-33-8 Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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The invention relates to compound of formula (I): wherein:represents a single or double bond,R0 represents hydrogen or hydroxy or alkoxy,R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or ?wherein m represents an integer such that 13 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl,X represents oxygen or sulphur or ?CH2? or ?CH2?CH2?,Ar represents aryl, heteroaryl or arylalkyl,its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid.Medicinal products containing the same are useful in the treatment of cancer.

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

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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.Read on for other articles about 22013-33-8Application of 22013-33-8“.

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A series of new acridines has been prepared by cyclodehydration of N-(2,3-dihydro-1,4-benzodioxin-6-yl)anthranilic acid in acidic media following classical procedures. All these compounds have in common a dioxygenated ring fused to the acridine. The tetracyclic system possesses a linear or angular structure formed by intramolecular cyclisation. The last ring and the substituent of the system modify, in an interesting way, the antitumor activity of acridines. Several of the studied compounds displayed significant cytotoxic activity (inhibition of L1210 and HT-29 cell proliferation). The most cytotoxic compound 13a, shows more activity than m-AMSA in inhibiting L1210 and HT-29 cell proliferation and this compound has been selected as a development candidate for further evaluation. The activity results also indicate that the new 11-O-substituted compounds are of considerable interest with high levels of cytotoxic activity. The angular or non-linear dioxinoacridine 10 was equiactive with the linear structure 7. Pentacyclic analogues (14 and 15) were more cytotoxic than the tetracyclic compounds (up to twofold).

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

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We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 22013-33-8, and how the biochemistry of the body works.Electric Literature of 22013-33-8

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The present invention relates to a novel 1H-pyrazolopyridine derivative and a pharmaceutical composition containing the same. The 1H-pyrazolopyridine derivative and the pharmaceutical composition containing the same can be usefully used for the prevention or treatment of autoimmune diseases or cancer.

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

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A chemical genomic screen of an in-house library of small molecule heterocycles was carried out using Xenopus laevis embryos. This led to the identification of N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-4-methoxyaniline (1c), which elicits loss of pigmentation in melanophores and the retinal pigment epithelium (RPE) of developing embryos, independent of the developmental stage of initial exposure. The phenotype was reversible, since pigmentation returned upon compound removal while analysis of neural crest cell markers (Pax7) and melanophore markers (Dct/Xtrp2) revealed that both neural crest precursors and fully differentiated melanophores were present in the dithiazole 1c treated embryos. A subsequent focused structure-activity relationship (SAR) study identified the more active dithiazole 4-benzyloxy-N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-aniline (1l) and the need for a chlorine substituent at the dithiazole C-4 position. Both the initial chemical genomic screen and the focused SAR study highlighted the toxicity of (dithiazolylidene)aminoazines, and also of methoxyaniline (anisidine) analogues that hosted strong electron-withdrawing or electronegative substituents or acidic hydroxyl groups on the anisidine moiety. This study suggests that 1,2,3-dithiazoles can act as reversible melanin synthesis inhibitors, revealing a new biological activity for this class of compounds. The inhibition of melanin synthesis is medically relevant as a potential treatment for pigmentation disorders such as melasma.

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

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Future efforts will undeniably focus on the diversification of the new catalytic transformations. These may comprise an expansion of the substrate scope from aromatic and heteroaromatic compounds to other hydrocarbons. Keep reading other articles of 22013-33-8Electric Literature of 22013-33-8.

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A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

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

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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.Read on for other articles about 22013-33-8Electric Literature of 22013-33-8“.

The prevalence of solvent effects has motivated developing quantitative kinetic, spectroscopic, and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states. Electric Literature of 22013-33-8, 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

The present invention relates to novel inhibitors of protein kinase C epsilon (PKCepsilon) signaling, including in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these inhibitors, and their use in the treatment or prevention of disorders such as, e.g., a cardiovascular disorder, cardiac hypertrophy, heart failure, anxiety, pain, chronic pain, migraine, an allergy, an inflammatory disorder, an autoimmune disorder, diabetes, diabetic complications, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic neuropathy, cancer, metastatic cancer, drug-resistant cancer, stomach cancer, lung cancer, thyroid cancer, colon cancer, breast cancer, a neurological disorder, Alzheimer’s disease, Parkinson’s disease, bipolar disorder, stroke, alopecia, or alcoholism.

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

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Novel 3,1-benzoxazinones, 3,1-benzothiazinones and 4-alkoxyquinazolines have been synthesized via N-aryl-1,2,3-dithiazoles derivatives. The antibacterial and antifungal activity of these compounds were measured; the dithiazoles are significantly active against fungi.

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

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We present a convenient synthesis of novel heteroaryl-fused 3-oxo-1,4-thiazepine-5-carboxamides and 5-oxo-1,4-thiazepine-3-carboxamides using a modification of four-component Ugi condensation. We demonstrate the usefulness and versatility of the developed approach for the synthesis of variously substituted compounds and discuss the scope and limitations of the chemistry involved.

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

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Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

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