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Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors

A useful and rapid access to libraries of N-arylbenzo[b]thieno[3,2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues was designed and optimized for the first time via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with N?-(2-cyanoaryl)-N,N- dimethylformimidamides obtained by reaction of thiophene precursors with dimethylformamide dimethylacetal. The inhibitory potency of the final products against five protein kinases (CDK5/p25, CK1delta/epsilon, GSK3alpha/beta, DYRK1A and CLK1) was estimated. N-arylpyrido[3?,2?:4,5]thieno[3,2-d] pyrimidin-4-amine series of compounds (4a-j) turned out to be particularly promising for the development of new pharmacological inhibitors of CK1 and CLK1 kinases.

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

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Copper-promoted sandmeyer difluoromethylthiolation of aryl and heteroaryl diazonium salts

An efficient copper-promoted difluoromethylthiolation of aryl and heteroaryl diazonium salts is described. The reaction is conducted under mild reaction conditions and various functional groups were compatible. In addition, reactions of heteroaryl diazonium salts such as pyridyl, quinolinyl, benzothiazolyl, thiophenyl, carbazolyl, and pyrazolyl diazonium salts occurred smoothly to afford the medicinally important difluoromethylthiolated heteroarenes. Furthermore, a more practical one-pot direct diazotization and difluoromethylthiolation protocol was developed, and it converts the aniline derivatives into difluoromethylthiolated arenes. The utility of the method is demonstrated by difluoromethylthiolation of a number of natural products and drug molecules. A dose of salt: The title reaction is conducted under mild reaction conditions and various functional groups are compatible. (Hetero)aryl diazonium salts reacted smoothly to afford the medicinally important difluoromethylthiolated (hetero)arenes. A practical one-pot direct diazotization and difluoromethylthiolation protocol was developed for aniline derivatives to generate difluoromethylthiolated arenes.

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

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BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

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

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Discovery of novel guanidinophenylpyrazole human acrosin inhibitors by molecular hybridization

Human acrosin is a promising target for male contraceptives. A series of novel guanidinophenylpyrazole derivatives were rationally designed by molecular hybridization of the phenylpyrazole and guanidinobenzoate inhibitors. Most of the target compounds showed potent human acrosin inhibitory activities. In particular, compound F3 was a highly active human acrosin inhibitor (IC50 = 1.26 muM) with good selectivity over trypsin. Molecular docking studies revealed that compound F3 formed hydrophobic and hydrogen bonding interactions with the active site of human acrosin. Compound F3 represents a promising lead compound for the development of novel male contraceptives.

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

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Design, synthesis and evaluation of pyrazole bearing alpha-aminophosphonate derivatives as potential acetylcholinesterase inhibitors against Alzheimer’s disease

A series of novel scaffold of N-substituted pyrazole derived alpha-aminophosphonates were designed, synthesized and evaluated for their anti-cholinesterase activity. Porcine pancreatic lipase (PPL) was used as a catalyst for the organic transformation. Compounds 4ah and 4bh proved to be more potent than the standard drug tacrine, rivastigmine and galantamine for AChE inhibition activity with IC50 value between 0.055 ¡À 0.143 muM and 0.017 ¡À 0.02 muM respectively. BuChE activity of the synthesized derivatives possessed moderate to weak inhibition potency. 4bh shows a comparable activity to Rivastigmine against BuChE (IC50 = 6.331 ¡À 0.17). The compounds did not show any cytotoxicity against HEK-293 cells when compared to standard drugs. Cell viability assay using N2a cell showed compounds 4ah and 4bh showed comparable results to positive control rivastigmine. In addition, these compounds showed promising antioxidant activities against DPPH and H2O2 scavenging. Both 4ah and 4bh showed mixed-type inhibition which supported by molecular docking studies by acting as a dual site inhibitor. The predicted ADME showed good pharmacokinetics as predicted by QikProp. DNA cleavage studies and DNA protection assay of active compounds were also performed. 4bh did not show any damage to DNA and was protective in nature.

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

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LATE SV40 (LSF) INHIBITORS

The present invention is directed to compositions, methods and kits for treatment of cancer, e.g. hepatocellular carcinoma (HCC). In some embodiments, the present invention discloses the use of a small-molecule compounds of Formula (I)-(V) to inhibit tubulin methylation or to modulate chromatin or cytoskeleton modification in a cell.

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

Top Picks: new discover of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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The transformation of simple hydrocarbons into more complex and valuable products has revolutionised modern synthetic chemistry. This type of reactivity has quickly become one of the cornerstones of modern catalysis.Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, In a article, mentioned the application of 22013-33-8, molecular formula is C8H9NO2

Potential Anticancer Benzo-naphthyridones with Fused Rings: a Theoretical Model for Predicting Orientation in the Cyclization of Intermediates

Synthesis of benzo[b]-1,8-naphthyridine-5-ones with fused ring from halonicotinic acids and amino-substituted benzoheterocycles, leads either to an isomeric mixture or to single isomers. MO calculations conducted on the starting amino-substituted benzoheterocycles, allow predictions of the derivative(s) to be obtained. Some selected compounds belonging to this series were screened in vitro against several human tumor cell lines.

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

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AMINOINDANE COMPOUNDS AND USE THEREOF IN TREATING PAIN

The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine

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

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Synthesis of new 3-phenylquinazolin-4(3H)-one derivatives as potent antibacterial agents effective against methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA)

Occurrence of infections due to the drug resistant Staphylococcus aureus is on rise necessitating the need for rapid development of new antibacterial agents. In our present work, a series of new 3-phenylquinazolin-4(3H)-one derivatives were designed, synthesized and evaluated for their antibacterial activity against ESKAP (E. coli, S. aureus, K. pneumoniae, A. baumannii, P. aeroginosa) pathogen panel and pathogenic mycobacterial strains. The study revealed that compounds 4a, 4c, 4e, 4f, 4g, 4i, 4o and 4p exhibited selective and potent inhibitory activity against Staphylococcus aureus with MIC values in the range of 0.125?8 mug/mL. Further, the compounds 4c, 4e and 4g were found to be non toxic to Vero cells (CC50 = >10?>100 mug/mL) and exhibited favourable selectivity index (SI = 40?>200). The compounds 4c, 4e and 4g also showed potent inhibitory activity against various MDR-S. aureus including VRSA. The promising results obtained indicated the potential use of the above series of compounds as promising antibacterial agents for the treatment of multidrug resistant Staphylococcus aureus infections.

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

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General rhodium-catalyzed oxidative cross-coupling reactions between anilines: Synthesis of unsymmetrical 2,2?-diaminobiaryls

Described herein is a dual chelation-assisted RhCl3-catalyzed oxidative C-H/C-H cross-coupling reaction of aniline derivatives. The highlight of this methodology is the chemo- and regioselective cross-coupling between electronically similar substrates, which represents a highly challenging task in oxidative Ar-H/Ar-H cross-coupling reactions. Furthermore, this Cp?-free catalytic reaction tolerates a range of functional groups and requires only a low molar ratio of coupling partners. These features expedite the synthesis of unsymmetrical 2,2?-diaminobiaryls.

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