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

Bibliographic Details
Title: Ultrasound-Promoted Synthesis of 3-(Thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carboximidamides and Anticancer Activity Evaluation in Leukemia Cell Lines
Authors: Santos, Eric F. S. dos, Cury, Nathália M., Nascimento, Tainara A. do, Raminelli, Cristiano, Casagrande, Gleison A., Pereira, Claudio M. P., Simionatto, Euclésio, Yunes, José A., Pizzuti, Lucas
Source: Journal of the Brazilian Chemical Society. February 2017 28(2)
Publisher Information: Sociedade Brasileira de Química, 2017.
Publication Year: 2017
Subject Terms: amidinopyrazole, pyrazoline, cytotoxic activity, leukemia, ultrasonic irradiation
More Details: 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.
Document Type: article
File Description: text/html
Language: English
ISSN: 0103-5053
DOI: 10.5935/0103-5053.20160166
Access URL: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532017000200217
Rights: info:eu-repo/semantics/openAccess
Accession Number: edssci.S0103.50532017000200217
Database: SciELO
More Details
ISSN:01035053
DOI:10.5935/0103-5053.20160166
Published in:Journal of the Brazilian Chemical Society
Language:English