Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine.
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.
Fernandes
Iva
I
CIQUP, Departamento de Química, Faculdade de Ciências, Universidade do Porto, P-4169-007 Porto, Portugal.
Vale
Nuno
N
de Freitas
Victor
V
Moreira
Rui
R
Mateus
Nuno
N
Gomes
Paula
P
D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D018938:Caco-2 Cells; D019073:HT29 Cells; D006801:Humans; D048289:Imidazolidines / Q000737:chemistry* / Q000494:pharmacology; D011319:Primaquine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000962:Antimalarials; D000970:Antineoplastic Agents; D048289:Imidazolidines; D011319:Primaquine