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Novel imidazo[1,2- a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities
Ist Teil von
European journal of medicinal chemistry, 2008-11, Vol.43 (11), p.2505-2517
Ort / Verlag
Kidlington: Elsevier Masson SAS
Erscheinungsjahr
2008
Quelle
ScienceDirect
Beschreibungen/Notizen
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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