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Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Nonsteroidal Anti-Inflammatory Drugs (CROSBI ID 146384)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Rajić, Zrinka ; Butula, Ivan ; Zorc, Branka ; Kraljević Pavelić, Sandra ; Hock, Karlo ; Pavelić, Krešimir ; Naesens, Lieve ; De Clercq, Erik ; Balzarini, Jan ; Przyborowska, Monika et al. Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Nonsteroidal Anti-Inflammatory Drugs // Chemical biology & drug design, 73 (2009), 3; 328-338. doi: 10.1111/j.1747-0285.2009.00774.x

Podaci o odgovornosti

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

engleski

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

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.

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

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Podaci o izdanju

73 (3)

2009.

328-338

objavljeno

1747-0277

1747-0285

10.1111/j.1747-0285.2009.00774.x

Povezanost rada

Kemija

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