9 documents found, page 1 of 1
Synthesis and antimetastatic activity evaluation of cinnamic acid derivatives c...
Lima, Graziela Domingues de Almeida; Rodrigues, Michelle Peixoto; Moreira, Gabriela Alves; Mendes, Tiago Antônio de Oliveira; Siqueira, Raoni PaisIt is herein described the preparation and evaluation of antimetastatic activity of twenty-six cinnamic acid derivatives containing 1,2,3-triazolic portions. The compounds were prepared using as the key step the Copper(I)-catalyzed azide (A)-alkyne (A) cycloaddition (C) (CuAAC reaction), also known as click reaction, between alkynylated cinnamic acid derivatives and different benzyl azides. The reactions were c...
Antimetastatic effect of the pharmacological inhibition of serine/arginine-rich...
Moreira, Gabriela Alves; Lima, Graziela Domingues de Almeida; Siqueira, Raoni Pais; Barros, Marcus Vinícius de AndradeThe Serine/arginine-rich protein kinases (SRPK) are involved in pre-mRNA splicing control through the phosphorylation of the SR protein family of splicing factors. Over the last years, several studies have shown the relevance of SRPK for human cancers and their potential as promising drug targets. In this context, we have previously selected three trifluoromethyl arylamides (named here as SRVIC24, SRVIC30 and S...
Síntese e avaliação da atividade citotóxica de derivados do eugenol contendo nú...
Gazolla, Poliana Aparecida Rodrigues; Teixeira, Róbson Ricardo; Silva, Adalberto Manoel da; Vaz, Boniek Gontijo; Vasconcelos, Géssica AdrianaEugenol is an aromatic compound found in several plant species. It presents important biological activities including cytotoxicity. In this paper, it is described the synthesis and the evaluation of the cytotoxic activity of eugenol derivatives bearing 1,2,3-triazole functionalities. Eugenol, extracted via hydrodistillation from dried flower buds of Eugenia caryophyllata (=Syzygium aromaticum), was submitted to...
Trifluoromethyl arylamides with antileukemia effect and intracellular inhibitor...
Siqueira, Raoni Pais; Barros, Marcus Vinícius de Andrade; Barbosa, Éverton de Almeida Alves; Onofre, Thiago Souza; Gonçalves, Victor Hugo SousaThe serine/arginine-rich protein kinases (SRPKs) have frequently been found with altered activity in a number of cancers, suggesting they could serve as potential therapeutic targets in oncology. Here we describe the synthesis of a series of twenty-two trifluoromethyl arylamides based on the known SRPKs inhibitor N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide (SRPIN340) and the evaluation of th...
Synthesis, molecular properties prediction and cytotoxic screening of 3-(2-aryl...
Maia, Angélica Faleiros da Silva; Siqueira, Raoni Pais; Oliveira, Fabrício Marques de; Ferreira, Joana Gasperazzo; Silva, Silma Francielle daIn the present investigation, a collection of nineteen 3-(2-aryl-2-oxoethyl)isobenzofuran-1(3H)-ones was synthesized and screened for their cytotoxic activity against a panel of three leukemia cancer cell lines. The compounds were prepared via ZrOCl2·8H2O catalyzed condensation reactions between phthalaldehydic acid and different acetophenones. The reactions were carried out free of solvent and the isobenzofura...
Serine/arginine protein kinase (SRPK) inhibition as a potential therapeutic str...
Siqueira, Raoni PaisCoordenação de Aperfeiçoamento de Pessoal de Nível Superior; Serine/Arginine protein kinases (SRPKs) são componentes chave da maquinaria de splicing através da regulação por fosforilação das proteínas SR, as quais são cruciais para a seleção dos sítios de splicing alternativo. Entretanto, as SRPKs são frequentemente encontradas superexpressas ou com atividade alterada em diversos tipos de cânceres, inclusive em...
Potential antileukemia effect and structural analyses of SRPK inhibition by N-(...
Siqueira, Raoni Pais; Barbosa, Éverton de Almeida Alves; Polêto, Marcelo Depólo; Righetto, Germanna Lima; Seraphim, Thiago VargasDysregulation of pre-mRNA splicing machinery activity has been related to the biogenesis of several diseases. The serine/arginine-rich protein kinase family (SRPKs) plays a critical role in regulating pre-mRNA splicing events through the extensive phosphorylation of splicing factors from the family of serine/arginine-rich proteins (SR proteins). Previous investigations have described the overexpression of SRPK1...
Splicing regulators and their roles in cancer biology and therapy
Silva, Maria Roméria da; Moreira, Gabriela Alves; Silva, Ronni Anderson Gonçalves da; Barbosa, Éverton de Almeida Alves; Siqueira, Raoni PaisAlternative splicing allows cells to expand the encoding potential of their genomes. In this elegant mechanism, a single gene can yield protein isoforms with even antagonistic functions depending on the cellular physiological context. Alterations in splicing regulatory factors activity in cancer cells, however, can generate an abnormal protein expression pattern that promotes growth, survival, and other process...
Chemical constituents and an alternative medicinal veterinary herbal soap made ...
Andrade, Flávia Inoue; Purgato, Gislaine Aparecida; Maia, Thalita de Faria; Siqueira, Raoni Pais; Lima, Sâmia; Diaz, Gaspar; Diaz, Marisa Alves NogueiraUpon undergoing biomonitoring, the most active dichloromethane extract retrieved from Senna macranthera roots led to the isolation of three main compounds: emodine, physione, and chrysophanol. In this sequence, these compounds revealed a potential antibacterial activity against Staphylococcus aureus strains isolated from animals with mastitis infections with minimum inhibitory concentration (MIC) values of 20, ...