Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6914-7. doi: 10.1016/j.bmcl.2009.10.081.

Iva Fernandes ¹, Nuno Vale, Victor de Freitas, Rui Moreira, Nuno Mateus, Paula Gomes

Affiliations

Affiliation

1 CIQUP, Departamento de Química, Faculdade de Ciências, Universidade do Porto, P-4169-007 Porto, Portugal.

PMID: 19896373 DOI: 10.1016/j.bmcl.2009.10.081

Abstract

The growth inhibitory activity of imidazoquines, antimalarial imidazolidin-4-ones derived from primaquine, on human Cancer cell lines HT-29, Caco-2, and MCF-7 has been evaluated. Primaquine, N-dipeptidyl-primaquine derivatives, and Other quinolines have been included in the study for comparison purposes. Primaquine and some of its derivatives were significantly active against the MCF-7 human breast Cancer cell line, so these compounds might represent useful leads targeted at the development of novel specific agents against breast Cancer. Conversely, all compounds were generally inactive against HT-29, with only one of the imidazoquines having IC(50) below 50 microM. Activities against the Caco-2 cell line were modest and did not follow any defined trend.

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