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2.
Bioorg Med Chem Lett ; 49: 128264, 2021 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-34280408

RESUMO

In the present study we synthesized new methoxy derivatives of trans 2,3-diaryl-2,3-dihydrobenzofurans, starting from suitable trans 2,3-diaryloxiranes, using regio- and stereoselective nucleophilic oxiranyl ring-opening reactions. The compounds were tested as anti-inflammatories in U937 cells. All compounds showed a significant role in inhibiting the NF-κB pathway and were able to restore normal ROS and NO level upon LPS activation. Moreover, regarding inhibition of ACLY, enantioenriched (50% ee) 7a50 showed more potency than the racemic counterpart 7arac, together with a higher reduction of prostaglandin E2 production, thus suggesting a stereoselective interaction in this pathway.


Assuntos
Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , ATP Citrato (pro-S)-Liase/antagonistas & inibidores , Anti-Inflamatórios/síntese química , Benzofuranos/síntese química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Humanos , Estrutura Molecular , Óxido Nítrico/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição RelA/metabolismo , Células U937
3.
Fungal Genet Biol ; 21(3): 348-63, 1997 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-9290248

RESUMO

In the Neurospora Genome Project at the University of New Mexico, expressed sequence tags (ESTs) corresponding to three stages of the life cycle of the filamentous fungus Neurospora crassa are being analyzed. The results of a pilot project to identify expressed genes and determine their patterns of expression are presented. 1,865 partial complementary DNA (cDNA) sequences for 1,409 clones were determined using single-pass sequencing. Contig analysis allowed the identification of 838 unique ESTs and 156 ESTs present in multiple cDNA clones. For about 34% of the sequences, highly or moderately significant matches to sequences (of known and unknown function) in the NCBI database were detected. Approximately 56% of the ESTs showed no similarity to previously identified genes. Among genes with assigned function, about 43.3% were involved in metabolism, 32.9% in protein synthesis and 8.4% in RNA synthesis. Fewer were involved in defense (6%), cell signalling (3.4%), cell structure (3.4%) and cell division (2.6%).


Assuntos
Proteínas Fúngicas/genética , Genes Fúngicos , Neurospora crassa/genética , Neurospora crassa/fisiologia , Sequência de Aminoácidos , Sequência de Bases , Divisão Celular , DNA Complementar/química , Proteínas Fúngicas/biossíntese , Expressão Gênica , Biblioteca Gênica , Genoma Fúngico , Dados de Sequência Molecular , Neurospora crassa/citologia , RNA Mensageiro/biossíntese
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