Naslov
Antioxidative and antiproliferative activities of novel pyrido[1,2-a]benzimidazoles

Autori
Tireli, Martina ; Starčević, Kristina ; Martinović, Tamara ; Kraljević Pavelić, Sandra ; Karminski-Zamola, Grace ; Hranjec, Marijana

Izvornik
Molecular diversity (1381-1991) 21 (2017), 1; 201-210

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
pyrido[1 ; 2-a]benzimidazoles ; amides ; antiproliferative activity ; antioxidative activity ; cyclization

Sažetak
A series of pyrido[1, 2-a]benzimidazoles has been designed, novel examples synthesized and evaluated for their potential antiproliferative activity against four human tumor cell lines - cervical (HeLa), colorectal (SW620), breast (MCF-7) and hepatocellular carcinoma (HepG2). In addition, their antioxidative potency has been evaluated by in vitro spectrophotometric assays. Preliminary structure- activity relationships among the synthesized compounds are discussed. Evaluation of their antioxidative capacity has shown that two compounds (25 and 26) possess promising reducing characteristics and free-radical scavenging activity. Selective antiproliferative effect in the single- digit micromolar range was observed for compound 25 on MCF-7 (IC50 = 6 µM) and HeLa (IC50 = 8 µM) cell lines, comparable to the standards 5-fluorouracil and cisplatin. The combination of the radical scavenging activity and antiproliferative activity of compound 25 positions this compound as a potential lead candidate for further optimisation.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti

POVEZANOST RADA