Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Non-steroidal Anti-inflammatory Drugs

Zrinka Rajic , Ivan Butula , Branka Zorc , Sandra Kraljevic Pavelic , Karlo Hock , Kresimir Pavelic , Lieve Naesens , Erik De Clercq , Jan Balzarini , Monika Przyborowska , Tadeusz Ossowski , Mladen Mintas


Non‐steroidal 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 (100μm) 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 10μm. Among those three compounds, only compound 3b showed a selective cytostatic effect on HeLa in comparison with normal fibroblasts.
Author Zrinka Rajic
Zrinka Rajic,,
, Ivan Butula
Ivan Butula,,
, Branka Zorc
Branka Zorc,,
, Sandra Kraljevic Pavelic
Sandra Kraljevic Pavelic,,
, Karlo Hock
Karlo Hock,,
, Kresimir Pavelic
Kresimir Pavelic,,
, Lieve Naesens
Lieve Naesens,,
, Erik De Clercq
Erik De Clercq,,
, Jan Balzarini
Jan Balzarini,,
, Monika Przyborowska (FCh / DACh)
Monika Przyborowska,,
- Department of Analytical Chemistry
et al.`
Journal seriesChemical Biology & Drug Design, ISSN 1747-0277, (A 25 pkt)
Issue year2009
Publication size in sheets0.5
Keywords in Englishantitumor agents, NSAID hydroxamic acids, tumor cells, effectors of apoptosis
Languageen angielski
Score (nominal)25
Publication indicators WoS Impact Factor: 2009 = 2.473 (2) - 2009=2.683 (5)
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* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.