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izvor podataka: crosbi

Primaquine homodimers as potential antiplasmodial and anticancer agents (CROSBI ID 269518)

Prilog u časopisu | kratko priopćenje | međunarodna recenzija

Pavić, Kristina ; Rubinić, Barbara ; Rajić, Zrinka ; Fontinha, Diana ; Prudêncio, Miguel ; Uzelac, Lidija ; Kralj, Marijeta ; Held, Jana ; Zorc, Branka Primaquine homodimers as potential antiplasmodial and anticancer agents // Bioorganic & medicinal chemistry letters, 29 (2019), 126614, 5. doi: 10.1016/j.bmcl.2019.08.018

Podaci o odgovornosti

Pavić, Kristina ; Rubinić, Barbara ; Rajić, Zrinka ; Fontinha, Diana ; Prudêncio, Miguel ; Uzelac, Lidija ; Kralj, Marijeta ; Held, Jana ; Zorc, Branka

engleski

Primaquine homodimers as potential antiplasmodial and anticancer agents

Primaquine homodimers, e.g. symmetric PQ-diamides of dicarboxylic acids containing 4 to 8 carbon atoms, were evaluated against Plasmodium berghei hepatic stages and P. falciparum blood stages, as well as against three cancer cell lines. Novel PQ-homodimers exerted much higher activity against hepatic stages, but less pronounced activity against blood stages in comparison to the parent drug. The submicromolar activity of succinic, fumaric and maleic derivatives against P. berghei was determined (IC50 values: 726.2, 198.1 and 358.4 nM, respectively). Our results indicated that the length and type of spacer between two PQ moieties highly modified the antiproliferative activities of PQ-homodimers. The general antiproliferative activity of the adipic and mesaconic derivatives against three cancer cell lines (MCF-7, HCT116, H 460) was observed (GI50 = 1.78–13.7 and 2.36–4.31 µM, respectively), but adipic derivative was less toxic to human embryonic kidney cells (HEK 293). High selectivity of fumaric and suberic derivatives against breast adenocarcinoma cell line MCF-7 was detected. These two compounds have shown no antiproliferative activity against other tumor cells and HEK 293.

Primaquine ; Homodimer ; Antiplasmodial activity ; Cytostatic activity

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Podaci o izdanju

29

2019.

126614

5

objavljeno

0960-894X

1464-3405

10.1016/j.bmcl.2019.08.018

Povezanost rada

Temeljne medicinske znanosti, Farmacija

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