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Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones |
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| Authors: | Ahn Gang Schifano-Faux Nadège Goossens Jean-François Baldeyrou Brigitte Couture Axel Grandclaudon Pierre Lansiaux Amélie Ryckebusch Adina |
| Affiliation: | a EA CMF 4478, Université Lille 1-Lille Nord de France, Bat C3(2), Cité Scientifique, 59655 Villeneuve d’Ascq Cedex, France b Laboratoire de Chimie Analytique, EA 4481, Université Lille 2-Lille Nord de France, 3 rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France c Inserm U837, Centre Oscar Lambret, Université Lille 2- Lille Nord de France, IRCL et IMPRT, 1 Place de Verdun, 59045 Lille Cedex, France d Ecole Nationale Supérieure de Chimie de Lille, Avenue Dimitri Mendeleïev, Cité Scientifique, BP 90108, 59652 Villeneuve d’Ascq Cedex, France |
| Abstract: | A number of mono- or diaminoalkylated indeno[1,2-c]isoquinolin-5,11-diones analogs of 1 were synthesized and evaluated for their DNA binding affinities, topoisomerase inhibition properties and antiproliferative activities against human cancer cell lines (HL60). Impact of the side chain connected to the aromatic D ring and to the N6 lactam position on the biological profile will be discussed. |
| Keywords: | Cancer DNA intercalators Topoisomerases Indenoisoquinolines |
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