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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

Synthesis and leishmanicidal activity of eugenol derivatives bearing 1,2,3-tria...

Teixeira, Róbson Ricardo; Gazolla, Poliana Aparecida Rodrigues; Silva, Adalberto Manoel da; Borsodi, Maria Paula Gonçalves; Bergmann, Bartira Rossi

In this paper, it is described the synthesis and the evaluation of the leishmanicidal activity of twenty-six eugenol derivatives bearing 1,2,3-triazole functionalities. The evaluation of the compounds on promastigotes of Leishmania amazonensis (WHOM/BR/75/Josefa) showed that eugenol derivatives present leishmanicidal activities with varying degrees of effectiveness. The most active compound, namely 4-(3-(4-ally...

Date: 2018   |   Origin: Oasisbr

Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents

Lopes, Marcela Silva; Suzuki, Brian Michio; Pereira, Glaécia Aparecida do Nascimento; Probst, Alexandra Christina; Ferreira, Rafaela Salgado

In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mut...

Date: 2018   |   Origin: Oasisbr

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