Novel Lipophilic Hydroxyurea Derivatives: Synthesis, Cytostatic and Antiviral Activity Evaluations
Identifieur interne : 001613 ( Main/Exploration ); précédent : 001612; suivant : 001614Novel Lipophilic Hydroxyurea Derivatives: Synthesis, Cytostatic and Antiviral Activity Evaluations
Auteurs : Ivana Perkovi [Croatie] ; Ivan Butula [Croatie] ; Branka Zorc [Croatie] ; Karlo Hock [Croatie] ; Sandra Kraljevi Paveli [Croatie] ; Krešimir Paveli [Croatie] ; Erik De Clercq [Belgique] ; Jan Balzarini [Belgique] ; Mladen Mintas [Croatie]Source :
- Chemical Biology & Drug Design [ 1747-0277 ] ; 2008-06.
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.
Url:
DOI: 10.1111/j.1747-0285.2008.00660.x
Affiliations:
- Belgique, Croatie
- Province du Brabant flamand, Région flamande
- Louvain
- Katholieke Universiteit Leuven
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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.</div></front></TEI><affiliations><list><country><li>Belgique</li><li>Croatie</li></country><region><li>Province du Brabant flamand</li><li>Région flamande</li></region><settlement><li>Louvain</li></settlement><orgName><li>Katholieke Universiteit Leuven</li></orgName></list><tree><country name="Croatie"><noRegion><name sortKey="Perkovi, Ivana" sort="Perkovi, Ivana" uniqKey="Perkovi I" first="Ivana" last="Perkovi">Ivana Perkovi</name></noRegion><name sortKey="Butula, Ivan" sort="Butula, Ivan" uniqKey="Butula I" first="Ivan" last="Butula">Ivan Butula</name><name sortKey="Hock, Karlo" sort="Hock, Karlo" uniqKey="Hock K" first="Karlo" last="Hock">Karlo Hock</name><name sortKey="Mintas, Mladen" sort="Mintas, Mladen" uniqKey="Mintas M" first="Mladen" last="Mintas">Mladen Mintas</name><name sortKey="Mintas, Mladen" sort="Mintas, Mladen" uniqKey="Mintas M" first="Mladen" last="Mintas">Mladen Mintas</name><name sortKey="Paveli, Kresimir" sort="Paveli, Kresimir" uniqKey="Paveli K" first="Krešimir" last="Paveli">Krešimir Paveli</name><name sortKey="Paveli, Sandra Kraljevi" sort="Paveli, Sandra Kraljevi" uniqKey="Paveli S" first="Sandra Kraljevi" last="Paveli">Sandra Kraljevi Paveli</name><name sortKey="Zorc, Branka" sort="Zorc, Branka" uniqKey="Zorc B" first="Branka" last="Zorc">Branka Zorc</name><name sortKey="Zorc, Branka" sort="Zorc, Branka" uniqKey="Zorc B" first="Branka" last="Zorc">Branka Zorc</name></country><country name="Belgique"><region name="Région flamande"><name sortKey="Clercq, Erik De" sort="Clercq, Erik De" uniqKey="Clercq E" first="Erik De" last="Clercq">Erik De Clercq</name></region><name sortKey="Balzarini, Jan" sort="Balzarini, Jan" uniqKey="Balzarini J" first="Jan" last="Balzarini">Jan Balzarini</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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