Naslov
Synthesis, cytostatic and anti-viral activity evaluation of the novel acyclic nucleoside analogues containing a sterically constrained (Z)-4-amino-2-butenyl moiety

Autori
Wittine, Karlo ; Benci, Krešimir ; Kraljević Pavelić, Sandra ; Pavelić, Krešimir ; Bratulić, Siniša ; Hock, Karlo ; Balzarini, Jan ; Mintas, Mladen

Izvornik
Medicinal chemistry research (1054-2523) 20 (2011), 3; 280-287

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

Ključne riječi
acyclic nucleoside analogues; purine and pyrimidine derivatives; cytostatic activity; antiviral activity

Sažetak
A series of the novel pyrimidine (3-6) and purine (12-15, 18-21) acyclic nucleoside analogues in which the sugar moiety was replaced by a sterically constrained Z-4-amino-, 4-aminohydrochloride-2-butenyl, or aliphatic 4-aminohydrochloride-2-butyl moiety were synthesized and evaluated for their antiviral and cytostatic activity potency. Cytostatic evaluation of the novel compounds on selected panel of human tumour cell lines showed that the majority of compounds exerted a non-specific antiproliferative effect at the highest tested concentration (i.e. 1 x 10-4 M) against all cell lines. Nevertheless, a rather moderate but selective antiproliferative effects on HeLa cell cultures in comparison to normal fibroblasts WI 38, was observed for compounds 15 and 21. No antiviral activity was observed, except for compounds 3, 4 and 5 that showed anti-HIV activity at 50% effective concentration ranging between 29 and 96 µM.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti

POVEZANOST RADA