Novel imidazo[1,2-a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities
摘要:
Novel imidazo[1,2-a]naphthyridinic systems 6a-15a and 6b-15b were obtained from Friedlander'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. (C) 2008 Elsevier Masson SAS. All rights reserved.
Novel imidazo[1,2-a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities
作者:Mounir Andaloussi、Emmanuel Moreau、Nicolas Masurier、Jacques Lacroix、René C. Gaudreault、Jean-Michel Chezal、Anas El Laghdach、Damien Canitrot、Eric Debiton、Jean-Claude Teulade、Olivier Chavignon
DOI:10.1016/j.ejmech.2008.02.017
日期:2008.11
Novel imidazo[1,2-a]naphthyridinic systems 6a-15a and 6b-15b were obtained from Friedlander'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. (C) 2008 Elsevier Masson SAS. All rights reserved.