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Novel imidazo[1,2-a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities

Abstract : Novel imidazo[1,2-a]naphthyridinic systems 6a-15a and 6b-15b were obtained from Friedländer's reaction in imidazo[1,2-a]pyridine series. Most of the compounds were evaluated for their antitumor activity in the NCIs in vitro human tumor cell line screening panel. Among them, pentacyclic derivatives 13b and 14a exhibited in vitro activity comparable to anticancer agent such as amsacrine. Their mechanism of cytotoxicity action was unrelated to poisoning or inhibiting abilities against topo1. On the contrary, we highlighted a direct intercalation of the drugs into DNA by electrophoresis on agarose gel.
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https://hal.archives-ouvertes.fr/hal-01677576
Contributor : Emmanuel Moreau <>
Submitted on : Monday, January 8, 2018 - 2:45:12 PM
Last modification on : Wednesday, March 4, 2020 - 11:26:01 AM

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Emmanuel Moreau, Mounir Andaloussi, Nicolas Masurier, Jacques Lacroix, René C Gaudreault, et al.. Novel imidazo[1,2-a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities. European Journal of Medicinal Chemistry, Elsevier, 2008, 43 (11), pp.2505 - 2517. ⟨10.1016/j.ejmech.2008.02.017⟩. ⟨hal-01677576⟩

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