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Pregled bibliografske jedinice broj: 1024073

Primaquine homodimers as potential antiplasmodial and anticancer agents


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 (međunarodna recenzija, kratko priopcenje, znanstveni)


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


Projekt / tema
HRZZ-IP-2014-09-1501 - Dizajniranje, sinteza i evaluacija derivata primakina, vorinostata i sorafeniba kao potencijalnih citostatika

Ustanove
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb

Citiraj ovu publikaciju

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 (međunarodna recenzija, kratko priopcenje, znanstveni)
Pavić, K., Rubinić, B., Rajić, Z., Fontinha, D., Prudêncio, M., Uzelac, L., Kralj, M., Held, J. & Zorc, B. (2019) Primaquine homodimers as potential antiplasmodial and anticancer agents. Bioorganic & medicinal chemistry letters, 29, 126614, 5 doi:10.1016/j.bmcl.2019.08.018.
@article{article, year = {2019}, pages = {5}, DOI = {10.1016/j.bmcl.2019.08.018}, chapter = {126614}, keywords = {Primaquine, Homodimer, Antiplasmodial activity, Cytostatic activity}, journal = {Bioorganic and medicinal chemistry letters}, doi = {10.1016/j.bmcl.2019.08.018}, volume = {29}, issn = {0960-894X}, title = {Primaquine homodimers as potential antiplasmodial and anticancer agents}, keyword = {Primaquine, Homodimer, Antiplasmodial activity, Cytostatic activity}, chapternumber = {126614} }

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


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