Naslov
Novel Lipophilic Hydroxyurea Derivatives: Synthesis, Cytostatic and Antiviral Activity Evaluations

Autori
Perković, Ivana ; Butula, Ivan ; Zorc, Branka ; Hock, Karlo ; Kraljević Pavelić, Sandra ; Pavelić, Krešimir ; De Clercq, Erik ; Balzarini, Jan ; Mintas, Mladen

Izvornik
Chemical biology & drug design (1747-0277) 71 (2008), 6; 546-553

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

Ključne riječi
antiviral activity; cytostatic activity; human tumor cell lines; hydroxyureas

Sažetak
The novel hydroxyurea derivatives of l- and d-amino acid amides 5a– l were prepared by aminolysis of N-(1-benzotriazolecarbonyl)-amino acid amides 4a– f with O-benzylhydroxylamine and N-methylhydroxylamine and evaluated for their antiviral and cytostatic activity against malignant tumor cell lines and normal human fibroblasts. Compounds 5a, 5c, 5e and 5k showed the highest antiproliferative effects against all tumor cell lines tested. The strongest non-specific cytostatic activities against HeLa cells were affected by compounds 5a, 5c, 5e and 5k on MCF-7 cells by 5c, 5e and 5k and MIA PACa-2 cells by 5c and 5k. Differential effects at micromolar concentrations were observed for compounds 5a, 5c, 5e, 5k and 5l in Hep G2 cells, for compounds 5c, 5e, 5k and 5l in PC-3 cells and for compounds 5e, 5k and 5l in SW 620 cells.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija

POVEZANOST RADA