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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 Andrade

The 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...

Date: 2019   |   Origin: Oasisbr

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 Adriana

Eugenol 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...

Date: 2019   |   Origin: Oasisbr

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 Sousa

The 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...

Date: 2018   |   Origin: Oasisbr

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