| Autor: |
Perin, Nataša, Martin Kleiner, Irena, Nhili, Raja, Laine, William, David-Cordonnier, Marie-Hélène, Vugrek, Oliver, Karminski-Zamola, Grace, Kralj, Marijeta, Hranjec, Marijana |
| Přispěvatelé: |
Hadžiev, Andrea, Blažeković, Zdenko |
| Jazyk: |
angličtina |
| Rok vydání: |
2013 |
| Předmět: |
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| Popis: |
The permanent and growing interest in the synthesis of azino fused benzimidazole derivatives, as a one of the most extensively studied classes of heterocyclic compounds, is a direct consequence of their diverse biological properties. We represent the synthesis of benzimidazo[1, 2-a]quinolines with amino side chains placed on quinoline nuclei in view of our continuing search and finding of new lead structures with chemotherapeutic activities.[1, 2] Amino-substituted compounds were synthesized by uncatalyzed microwave assisted amination from chloro-substituted precursor. All compounds showed prominent antiproliferative activity, while the length of the amino chains linked to the benzimidazo[1, 2-a]quinoline nuclei manipulated the antiproliferative activity. Although the majority of compounds were active in the submircomolar IC50 concentrations, we performed a series of additional experiments to shed more light on the mechanisms of action of the most active ones, including DNA binding, topoisomerases I and II inhibition, cell cycle perturbances and cellular localization. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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