Naslov
Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Nonsteroidal Anti-Inflammatory Drugs

Autori
Rajić, Zrinka ; Butula, Ivan ; Zorc, Branka ; Kraljević Pavelić, Sandra ; Hock, Karlo ; Pavelić, Krešimir ; Naesens, Lieve ; De Clercq, Erik ; Balzarini, Jan ; Przyborowska, Monika ; Ossowski, Tadeusz ; Mintas, Mladen

Izvornik
Chemical biology & drug design (1747-0277) 73 (2009), 3; 328-338

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

Ključne riječi
NSAID hydroxamic acids ; antitumor agents ; tumor cells: effectors of apoptosis

Sažetak
NSAID pharmacophores are interesting in designing potential anticancer drugs. Indeed, numerous experimental, epidemiologic, and clinical studies suggest that NSAIDs are promising anticancer drugs. Herein, NSAID hydroxamic acids 3a-i were prepared by a new synthetic procedure and evaluated for their antiviral and cytostatic activity against malignant tumor cell lines and normal human fibroblasts (WI38). Antiviral activity evaluation results indicated that 3f had only a minor activity against the influenza virus A/H1N1 subtype with a selectivity index of 7– 10. On the other hand, the results of the in vitro cytostatic activity evaluations revealed that the majority of NSAID hydroxamic acid derivatives 3a-i exhibited a strong non-specific antiproliferative effect at the highest concentration (100 µ ; ; ; M) on the tested cell line panel. Only compounds 3b, 3e and 3i exerted a differential dose-dependent inhibitory activity against the growth of HeLa cells (p < 0.05) at concentration 10 µ ; ; ; M. Among those three compounds, only compound 3b showed a selective cytostatic effect on HeLa in comparison to normal fibroblasts.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA