European journal of medicinal chemistry, 2008-11, Vol.43 (11), p.2505-2517
2008
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Details
- Autor(en) / Beteiligte
- Titel
- 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. [Display omitted]
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0223-5234eISSN: 1768-3254DOI: 10.1016/j.ejmech.2008.02.017Titel-ID: cdi_hal_primary_oai_HAL_hal_01677576v1
- Format
- –
- Schlagworte
- Antineoplastic agents, Benzoimidazonaphthyridine, Biological and medical sciences, Cell Line, Tumor, Cell Proliferation - drug effects, Chemical Sciences, Coordination chemistry, DNA - chemistry, DNA-intercalator, Friedländer's reaction, General aspects, Humans, Imidazo[1,2- a]pyridine, Imidazoles - chemistry, Imidazonaphthonaphthyridine, Imidazonaphthyridine, Intercalating Agents - chemical synthesis, Intercalating Agents - chemistry, Intercalating Agents - pharmacology, Medical sciences, Medicinal Chemistry, Molecular Structure, Naphthyridines - chemical synthesis, Naphthyridines - chemistry, Naphthyridines - pharmacology, Organic chemistry, Pharmacology. Drug treatments, Radiochemistry, Structure-Activity Relationship