Novel lipophilic hydroxyurea derivatives: Synthesis, cytostatic and antiviral activity evaluations

Perkovic, Ivana, Butula, Ivan, Zorc, Branka, Hock, Karlo, Pavelic, Sandra, Pavelic, Kresimir, de Clercq, Erik, Balzarini, Jan and Mintas, Mladen (2008) Novel lipophilic hydroxyurea derivatives: Synthesis, cytostatic and antiviral activity evaluations. Chemical Biology and Drug Design, 71 6: 546-553. doi:10.1111/j.1747-0285.2008.00660.x


Author Perkovic, Ivana
Butula, Ivan
Zorc, Branka
Hock, Karlo
Pavelic, Sandra
Pavelic, Kresimir
de Clercq, Erik
Balzarini, Jan
Mintas, Mladen
Title Novel lipophilic hydroxyurea derivatives: Synthesis, cytostatic and antiviral activity evaluations
Journal name Chemical Biology and Drug Design   Check publisher's open access policy
ISSN 1747-0277
1747-0285
Publication date 2008
Sub-type Article (original research)
DOI 10.1111/j.1747-0285.2008.00660.x
Open Access Status
Volume 71
Issue 6
Start page 546
End page 553
Total pages 8
Place of publication Malden, MA, United States
Publisher Wiley-Blackwell
Language eng
Abstract 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.
Keyword Antiviral activity
Cytostatic activity
Human tumor cell lines
Hydroxyureas
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Biological Sciences Publications
 
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Created: Wed, 27 Aug 2014, 14:18:35 EST by Gail Walter on behalf of School of Biological Sciences