Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis
| Autor: | Elena A. Rozhkova, Eerik M. Elias, Madhuri Manpadi, Jennifer D. Bettale, Snezna Rogelj, Alexander Kornienko, Nikolai M. Przheval’skii, Nikolai M. Evdokimov, Marcia A. Ogasawara, Igor V. Magedov |
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| Rok vydání: | 2007 |
| Předmět: |
Pyridones
Stereochemistry Clinical Biochemistry Substituent Pharmaceutical Science One-Step Apoptosis Jurkat cells Biochemistry Chemical synthesis Article HeLa Jurkat Cells Structure-Activity Relationship Meta chemistry.chemical_compound Drug Discovery Humans Structure–activity relationship Cytotoxicity Molecular Biology Cell Proliferation Malononitrile Bicyclic molecule biology Chemistry Organic Chemistry General Medicine biology.organism_classification Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:3872-3876 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.05.004 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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