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

• New series of N-acetyl and N-formyl-pyrazoline derivatives were synthesized.
• Pyrazoline derivates 6, 7 and 8 were obtained in acceptable to excellent yields.
• Compounds 7b and 8b–e showed potent antitumor activity with GI50 values of 10−7 M.
• Compound 7a showed a percentage of inhibition for Plasmodium falciparum of 50.8%.

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.

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