Pregled bibliografske jedinice broj: 1024073
Primaquine homodimers as potential antiplasmodial and anticancer agents
Primaquine homodimers as potential antiplasmodial and anticancer agents // Bioorganic & medicinal chemistry letters, 29 (2019), 126614, 5 doi:10.1016/j.bmcl.2019.08.018 (međunarodna recenzija, kratko priopcenje, znanstveni)
CROSBI ID: 1024073 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Primaquine homodimers as potential antiplasmodial and anticancer agents
Autori
Pavić, Kristina ; Rubinić, Barbara ; Rajić, Zrinka ; Fontinha, Diana ; Prudêncio, Miguel ; Uzelac, Lidija ; Kralj, Marijeta ; Held, Jana ; Zorc, Branka
Izvornik
Bioorganic & medicinal chemistry letters (0960-894X) 29
(2019);
126614, 5
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, kratko priopcenje, znanstveni
Ključne riječi
Primaquine ; Homodimer ; Antiplasmodial activity ; Cytostatic activity
Sažetak
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.
Izvorni jezik
Engleski
Znanstvena područja
Temeljne medicinske znanosti, Farmacija
POVEZANOST RADA
Projekti:
HRZZ-IP-2014-09-1501 - Dizajniranje, sinteza i evaluacija derivata primakina, vorinostata i sorafeniba kao potencijalnih citostatika (PVSderivatives) (HRZZ - 2014-09) ( CroRIS)
Ustanove:
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb
Profili:
Zrinka Rajić
(autor)
Branka Zorc
(autor)
Lidija Uzelac
(autor)
Kristina Pavić
(autor)
Marijeta Kralj
(autor)
Poveznice na cjeloviti tekst rada:
Pristup cjelovitom tekstu rada doi doi.org www.sciencedirect.com www.sciencedirect.comCitiraj ovu publikaciju:
Časopis indeksira:
- Current Contents Connect (CCC)
- Web of Science Core Collection (WoSCC)
- Science Citation Index Expanded (SCI-EXP)
- SCI-EXP, SSCI i/ili A&HCI
- Scopus
- MEDLINE