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1.
J Org Chem ; 83(5): 2993-2999, 2018 03 02.
Artigo em Inglês | MEDLINE | ID: mdl-29384672

RESUMO

A novel nickel-catalyzed C(sp3)-H arylation with nonactivated aryl fluorides is reported. The use of 1,3-bis(2,4,6-trimethylphenyl)imidazol-2-ylidene (IMes) as a ligand was found to be critical to the success of the reaction. This new method enables the synthesis of a wide range of triarylmethane derivatives.

2.
Molecules ; 23(8)2018 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-30071657

RESUMO

An efficient direct C(sp3)⁻H oxidation of diarylmethanes has been demonstrated by this study. This method employs environment-friendly O2 as an oxidant and is promoted by commercially available MN(SiMe3)2 [M = K, Na or Li], which provides a facile method for the synthesis of various diaryl ketones in excellent yields. This protocol is metal-free, mild and compatible with a number of functional groups on substrates.


Assuntos
Metano/química , Cetonas/química , Estrutura Molecular , Oxirredução
3.
Molecules ; 21(6)2016 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-27338322

RESUMO

A series of C2-symmetric chiral benzimidazolium salts, the precursor of N-heterocyclic carbene ligands, were designed and synthesized from 1,2-dibromobenzene. In situ prepared corresponding carbenes were tested in the asymmetric palladium-catalyzed intramolecular α-arylation of amides, affording chiral diarylmethanols with high yields and moderate enantioselectivities.


Assuntos
Amidas/química , Anestésicos Locais/química , Bromobenzenos/química , Indóis/química , Amidas/síntese química , Anestésicos Locais/síntese química , Bromobenzenos/síntese química , Catálise , Indóis/síntese química , Metano/análogos & derivados , Metano/química , Paládio/química , Sais/química , Estereoisomerismo
4.
Water Environ Res ; 92(12): 2095-2104, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32534479

RESUMO

The effect of static magnetic field (SMF) on azo dye Acid Red B (ARB) decolorization by the co-culture of activated sludge (AS) and two halotolerant yeasts Candida tropicalis A1 and Pichia occidentalis A2 was investigated. Microbial community structure of the co-cultures before and after treatment with SMFs of different intensity was analyzed through high-throughput sequencing and quantitative real-time polymerase chain reaction. The results showed that ARB decolorization efficiency by the defined co-culture was 1.25-fold to 1.51-fold elevated by 24.6-305.0 mT SMF. The best ARB decolorization and chemical oxygen demand (COD) removal performances by the co-culture were both achieved with 95.0 mT SMF. By contrast, biomass multiplication and sedimentation property of AS systems were not significantly influenced by SMF. Higher activities of intracellular key enzymes were determined (with 95.0 mT SMF) as responsible for better decolorization and COD removal performances. Bacteria belonging to Prolixibacter, Corynebacterium, Pelagibacterium, Demequina, and Sphingobacterium which might be responsible for azo dye decolorization and aromatic compounds biodegradation were significantly enriched only in presence of SMF. Fungal genera Candida and Pichia were also significantly enriched by 41.4-305.0 mT SMF, which might be responsible for higher treatment efficiency. PRACTITIONER POINTS: Dye degradation was enhanced by combination of static magnetic field and yeasts. Improvement of enzyme activity was responsible for better treatment performance. Putative azo-degrading-related bacteria and fungi were selectively enriched. High relative abundance of Candida and Pichia ensured high decolorization effects. Potentially effective improvement of bioprocesses for treating hypersaline wastewater.


Assuntos
Compostos Azo , Esgotos , Antagonistas de Receptores de Angiotensina , Inibidores da Enzima Conversora de Angiotensina , Biodegradação Ambiental , Corantes , Campos Magnéticos , Pichia
5.
Eur J Med Chem ; 121: 294-299, 2016 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-27266999

RESUMO

Bromodomains (BRDs) are protein interaction modules that selectively recognize ε -N-lysine residues, serving as key epigenetic readers and play a key role in epigenetic regulation of gene transcription. Bromodomain-containing protein 4 (BRD4), a protein containing two BRDs termed BD1 and BD2, has emerged as an attractive candidate for the development of inhibitors targeting gene transcription in several types of cancers. In this study, we made structural modifications of previously reported BRD4 inhibitors, to develop new chemical scaffold 3,4-dihydroquinoxalin-2(1H)-one. Four series of compounds (compounds 7-10) were synthesized, and the BRD4-inhibitory activity and anti-proliferative effect of these compounds were evaluated. We found compound 10d has remarkable anti-proliferative activities toward leukemia cells and could induce apoptosis by mitochondrial pathways. Notably, the analysis of molecular docking suggested that hydrophobic interaction was essential for compound 10d to bind to BD1. In conclusion, these results demonstrate the potential of compound 10d to be utilized as a BRD4 inhibitor with apoptosis inducing effect in future leukemia therapy.


Assuntos
Benzodiazepinonas/química , Benzodiazepinonas/farmacologia , Desenho de Fármacos , Proteínas Nucleares/antagonistas & inibidores , Fatores de Transcrição/antagonistas & inibidores , Benzodiazepinonas/metabolismo , Proteínas de Ciclo Celular , Linhagem Celular Tumoral , Avaliação Pré-Clínica de Medicamentos , Humanos , Simulação de Acoplamento Molecular , Proteínas Nucleares/química , Proteínas Nucleares/metabolismo , Conformação Proteica , Fatores de Transcrição/química , Fatores de Transcrição/metabolismo
6.
Carbohydr Polym ; 92(2): 1953-9, 2013 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-23399243

RESUMO

Zinc oxide nanoparticles have been successfully synthesized through a facile polyol method using bacterial cellulose (BC) as a template. BC membrane was used as a host matrix to introduce quantitatively Zn(2+) ions and then as nanoreactors to fabricate ZnO nanoparticles by hydrolysis of zinc acetate in a polyol medium. The influence of the concentration of zinc acetate and hydrolytic time on the morphologies and size of ZnO nanoparticles were investigated. The results indicated that the uniform spherical ZnO nanoparticles were incorporated into BC fibers. The resulting nanocomposites show good mechanical properties and high photocatalytic activity in the degradation of methyl orange.


Assuntos
Celulose/química , Gluconacetobacter xylinus/química , Glicóis/química , Nanopartículas/química , Óxido de Zinco/química , Óxido de Zinco/síntese química , Catálise , Técnicas de Química Sintética , Hidrólise , Fenômenos Mecânicos , Modelos Moleculares , Conformação Molecular , Processos Fotoquímicos , Porosidade , Temperatura , Acetato de Zinco/química
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