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(Referência obtida automaticamente do SciELO, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Ultrasound-Promoted Synthesis of 3-(Thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carboximidamides and Anticancer Activity Evaluation in Leukemia Cell Lines

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Autor(es):
Eric F. S. dos Santos ; Nathália M. Cury ; Tainara A. do Nascimento ; Cristiano Raminelli ; Gleison A. Casagrande ; Claudio M. P. Pereira ; Euclésio Simionatto ; José A. Yunes ; Lucas Pizzuti
Número total de Autores: 9
Tipo de documento: Artigo Científico
Fonte: Journal of the Brazilian Chemical Society; v. 28, n. 2, p. 217-224, Fev. 2017.
Resumo

3-(Thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carboximidamides were efficiently prepared through a cyclocondensation of thiophenylchalcones with aminoguanidine hydrochloride under ultrasonic conditions in the presence of KOH and ethanol as a green solvent in short reaction times (15-35 min) and good yields (62-95%). All compounds produced were evaluated against the human Jurkat and RS4;11 acute lymphoblastic leukemia cell lines of T- and B-cell origin, respectively, and the K562 myelogenous leukemia cell line. Six compounds presented half maximal inhibitory concentration (IC50) values around 15 µmol L-1 and five compounds presented IC50 values around 40 µmol L-1 for at least one of the three cell lines analyzed. One compound was not significantly cytotoxic, presenting IC50 value > 100 µmol L-1. (AU)

Processo FAPESP: 12/12802-1 - Mutações cooperantes, caracterização funcional e anticorpos contra o mutante do IL7R na leucemia linfóide aguda
Beneficiário:José Andrés Yunes
Linha de fomento: Auxílio à Pesquisa - Regular