Antiproliferative and apoptosis inducing properties of pyrano[3,2- c]pyridones accessible by a one-step multicomponent synthesis

4-Arylpyrano-[3,2- c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin-2(1H)-one with various substituted benzaldehydes and malononitrile. These heterocycles exhibit micromolar and submicromolar antiproliferative activity in HeLa and induce apoptosis in J...

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Published in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (14), p.3872-3876
Main Authors: Magedov, Igor V., Manpadi, Madhuri, Evdokimov, Nikolai M., Elias, Eerik M., Rozhkova, Elena, Ogasawara, Marcia A., Bettale, Jennifer D., Przheval’skii, Nikolai M., Rogelj, Snezna, Kornienko, Alexander
Format: Article
Language:eng ; rus
Subjects:
Apoptosis
Apoptosis - drug effects
Cell Proliferation - drug effects
Cytotoxicity
Heterocycles
Humans
Jurkat Cells
Multicomponent synthesis
Pyridones - pharmacology
Structure-Activity Relationship
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Summary:4-Arylpyrano-[3,2- c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin-2(1H)-one with various substituted benzaldehydes and malononitrile. These heterocycles exhibit micromolar and submicromolar antiproliferative activity in HeLa and induce apoptosis in Jurkat cell lines. Structure–activity studies performed on a small library of these compounds show a pronounced cytotoxicity enhancing effect of the bromo substituent at the meta position of the C4 aromatic moiety.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.05.004