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

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Data
2017
Autores
dos Santos, Eric F. S.
Cury, Nathalia M.
do Nascimento, Tainara A.
Raminelli, Cristiano [UNIFESP]
Casagrande, Gleison A.
Pereira, Claudio M. P.
Simionatto, Euclesio
Yunes, Jose A.
Pizzuti, Lucas
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Artigo
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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 mu mol L-1 and five compounds presented IC50 values around 40 mu mol L-1 for at least one of the three cell lines analyzed. One compound was not significantly cytotoxic, presenting IC50 value > 100 mu mol L- 1.
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Journal Of The Brazilian Chemical Society. Sao Paulo, v. 28, n. 2, p. 217-224 2017.
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