期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 67, 期 -, 页码 252-262出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.06.049
关键词
Pyrazolines; Chalcones; Cyclocondensation reaction; Antitumor and antimalarial activities
资金
- Colciencias, Universidad del Valle
- Universidad de Antioquia
A new series of N-acetyl and N-formyl-pyrazoline derivatives 6 and 7-8 were synthesized by cyclocondensation reaction of [(7-chloroquinolin-4-yl)amino]chalcones with hydrazine hydrate in acetic acid and hydrazine hydrate in formic acid respectively. These compounds were evaluated in vitro as antitumor and as antimalarial agents. Compounds 7b and 8b-e showed remarkable antitumor activity against cancer cell lines, with the most important GI(50) values ranging from 0.13 to 0.99 mu M. The best antimalarial response was observed for compound 7a with an inhibition percentage of 50.8% for Plasmodium falciparum, a hemolytic capacity of 3.2% and an IC50 of 14.1 mu g/mL. (C) 2013 Elsevier Masson SAS. All rights reserved.
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