Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 18, Pages 5791-5794Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.07.099
Keywords
4-Oxycoumarins; MCF-7; HL-60; U937; Neuro2a; Cytotoxic activity
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Funding
- Spanish Ministry [PS09/00501]
- Xunta de Galicia [09CSA030203PR]
- Italian Ministry [F21J10000010001]
- Regione Sardegna [PR-MAB-A2009-613]
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Coumarins are a large family of natural and synthetic compounds exerting different pharmacological effects, including cytotoxic, anti-inflammatory or antimicrobial. In the present communication we report the synthesis of a series of 12 diversely substituted 4-oxycoumarin derivatives including methoxy substituted 4-hydroxycoumarins, methyl, methoxy or unsubstituted 3-aryl-4-hydroxycoumarins and 4-benzyloxycoumarins and their anti-proliferative effects on breast adenocarcinoma cells (MCF-7), human promyelocytic leukemia cells (HL-60), human histiocytic lymphoma cells (U937) and mouse neuroblastoma cells (Neuro2a). The most potent bioactive molecule was the 4-hydroxy-5,7-dimethoxycoumarin (compound 1) which showed similar potency (IC50 0.2-2 mu M) in all cancer cell lines tested. This non-natural product reveals a simple bioactive scaffold which may be exploited in further studies. (c) 2012 Elsevier Ltd. All rights reserved.
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