期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 14, 页码 3872-3876出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.004
关键词
multicomponent synthesis; cytotoxicity; apoptosis; heterocycles
资金
- NCI NIH HHS [R15 CA099957-02, R15 CA099957] Funding Source: Medline
- NCRR NIH HHS [P20 RR016480, P20 RR016480-08] Funding Source: Medline
4-Arylpyrano-[3,2-c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin2(IH)-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. (C) 2007 Elsevier Ltd. All rights reserved.
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