1215290-47-3Relevant academic research and scientific papers
PPAR AGONIST COMPOSITIONS AND METHODS OF USE
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Page/Page column 55, (2010/07/09)
Method for treating or preventing a PPAR-responsive condition in a subject, comprising administering to the subject a PPAR agonist that comprises a 8-hydroxyquinoline-methylene-N- group in an amount effective to activate a PPAR polypeptide.
Structure-activity relationships and mechanism of action of antitumor bis 8-hydroxyquinoline substituted benzylamines
Madonna, Sébastien,Béclin, Christophe,Laras, Younes,Moret, Vincent,Marcowycz, Aline,Lamoral-Theys, Delphine,Dubois, Jacques,Barthelemy-Requin, Magali,Lenglet, Ga?lle,Depauw, Sabine,Cresteil, Thierry,Aubert, Geneviève,Monnier, Valérie,Kiss, Robert,David-Cordonnier, Marie-Hélène,Kraus, Jean-Louis
experimental part, p. 623 - 638 (2010/04/06)
A series of twenty six 8-hydroxyquinoline substituted amines, structurally related to compounds 2 and 3, were synthesized to evaluate the effects of structural changes on antitumor activity and understand their mechanism of action. The studies were performed on a wide variety of cancer cell lines within glioma and carcinoma models. The results obtained from chemical models and biological techniques such as microarrays suggest the following hypothesis that a quinone methide intermediate which does not react with DNA but which gives covalent protein thiol adducts. Micro-array analysis showed that the drugs induce the expression of a variety of stress related genes responsible for the cytotoxic and cytostatic effects in carcinoma and glioblastoma cells respectively. The described analogues could represent new promising anti-cancer candidates with specific action mechanisms, targeting accessible thiols from specific proteins and inducing potent anti-cancer effects.
