2. Academic Validation
  3. Synthesis of novel analogs of 2-pyrazoline obtained from [(7-chloroquinolin-4-yl)amino]chalcones and hydrazine as potential antitumor and antimalarial agents

Synthesis of novel analogs of 2-pyrazoline obtained from [(7-chloroquinolin-4-yl)amino]chalcones and hydrazine as potential antitumor and antimalarial agents

  • Eur J Med Chem. 2013 Sep:67:252-62. doi: 10.1016/j.ejmech.2013.06.049.
Braulio Insuasty 1,  Alba Montoya,  Diana Becerra,  Jairo Quiroga,  Rodrigo Abonia,  Sara Robledo,  Ivan Darío Vélez,  Yulieth Upegui,  Manuel Nogueras,  Justo Cobo
Affiliations

Affiliation

  • 1 Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A. A. 25360 Cali, Colombia. Electronic address: braulio.insuasty@correounivalle.edu.co.
PMID: 23871905 DOI: 10.1016/j.ejmech.2013.06.049
Abstract

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 GI50 values ranging from 0.13 to 0.99 μM. 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 μg/mL.

Keywords

Antitumor and antimalarial activities; Chalcones; Cyclocondensation reaction; Pyrazolines.

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