Camptothecin conjugated with DNA minor-groove binder netropsin: enhanced lactone stability, inhibition of human DNA topoisomerase I and antiproliferative activity.

Journal

Anticancer research

Auteurs

Membres identifiés du Cancéropôle Est :
Dr DEVY Jérôme , Pr NABIEV Igor

Tous les auteurs :
Sukhanova A, Grokhovsky S, Zhuze A, Devy J, Pluot M, Oleinikov V, Nabiev I

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/12894548

Résumé

The conjugates of camptothecin (CPT) with ligands possessing different DNA selectivity could be promising agents in cancer therapy affecting expression of specific genes by trapping DNA topoisomerase I (top I)-DNA complexes in a sequence-selective manner. Our recent data show that minor-groove binder netropsin (Nt) and its derivatives modulate the CPT-induced pattern of top I-mediated DNA cleavage. In an effort to develop a new molecule with good biological activity we have linked CPT with Nt and report here the first results of in vitro examination of the new compound.

Mots clés

Antineoplastic Agents, chemistry, Camptothecin, analogs & derivatives, Drug Stability, Enzyme Inhibitors, chemistry, Growth Inhibitors, chemistry, HT29 Cells, Humans, K562 Cells, Lactones, chemistry, Netropsin, analogs & derivatives, Topoisomerase I Inhibitors, Tumor Cells, Cultured

Référence

Anticancer Res.. ;23(3B):2609-15