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(Reference retrieved automatically from SciELO through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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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Author(s):
Eric F. S. dos Santos [1] ; Nathália M. Cury ; Tainara A. do Nascimento [3] ; Cristiano Raminelli [4] ; Gleison A. Casagrande [5] ; Claudio M. P. Pereira [6] ; Euclésio Simionatto [7] ; José A. Yunes ; Lucas Pizzuti [9]
Total Authors: 9
Affiliation:
[1] Universidade Federal da Grande Dourados. Grupo de Pesquisa em Síntese e Caracterização Molecular do MS - Brasil
[3] Universidade Federal da Grande Dourados. Grupo de Pesquisa em Síntese e Caracterização Molecular do MS - Brasil
[4] Universidade Federal de São Paulo. Departamento de Ciências Exatas e da Terra - Brasil
[5] Universidade Federal da Grande Dourados. Grupo de Pesquisa em Síntese e Caracterização Molecular do MS - Brasil
[6] Universidade Federal de Pelotas. Centro de Ciências Químicas, Farmacêuticas e dos Alimentos. Laboratório de Lipidômica e Bio-Orgânica - Brasil
[7] Universidade Estadual de Mato Grosso do Sul - Brasil
[9] Universidade Federal da Grande Dourados. Grupo de Pesquisa em Síntese e Caracterização Molecular do MS - Brasil
Total Affiliations: 9
Document type: Journal article
Source: Journal of the Brazilian Chemical Society; v. 28, n. 2, p. 217-224, 2017-02-00.
Abstract

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)

FAPESP's process: 12/12802-1 - Cooperating mutations, functional studies and antibodies against the mutant IL7R in acute lymphoblastic leukemia
Grantee:José Andrés Yunes
Support Opportunities: Regular Research Grants