期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 19, 页码 5171-5173出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.08.098
关键词
gamma-lactones; anticancer drugs; drug discovery; privileged structures; ring closing metathesis
资金
- Spanish MEC
- European Regional Development Fund [CTQ2005-09074-C0201/BQU]
- Canary Islands Government
- Fundacion Canaria de Investigacion y Salud [PI 1/06, PI 35/06]
A set of gamma-lactones alpha,beta-fused and beta,gamma-fused to carbocycles have been synthesized and evaluated for their in vitro antiproliferative activities using the human cancer cell lines SW1573 (lung), T-47D (breast) and WiDr (colon). The compounds are obtained by intramolecular ring closing metathesis of the corresponding dienes. Active compounds exhibited GI(50) values in the range 8-18 mu M. A structure-activity relationship is also discussed. (C) 2008 Elsevier Ltd. All rights reserved.
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