Primaquine homodimers as potential antiplasmodial and anticancer agents (CROSBI ID 269518)
Prilog u časopisu | kratko priopćenje | međunarodna recenzija
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