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.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antiprotozoal Agents / chemical synthesis
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Chalcones / chemistry*
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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Hydrazines / chemistry*
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Molecular Structure
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects*
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Structure-Activity Relationship
Substances
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((7-chloroquinolin-4-yl)amino)chalcone
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Antineoplastic Agents
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Antiprotozoal Agents
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Chalcones
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Hydrazines
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Pyrazoles
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hydrazine