Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 22, Pages 5234-5237Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.061
Keywords
Antimalarial; Abietane; Diterpene; Ferruginol; Dehydroabietylamine
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Funding
- Spanish Ministry of Science and Education
- Generalitat Valenciana
- American Lebanese Syrian Associated Charities (ALSAC) at St. Jude Children's Research Hospital
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The abietane-type diterpenoid (+)-ferruginol, a bioactive compound isolated from New Zealand's Miro tree (Podocarpus ferruginea), displays relevant pharmacological properties, including antimicrobial, cardioprotective, anti-oxidative, anti-plasmodial, leishmanicidal, anti-ulcerogenic, anti-inflammatory and anticancer. Herein, we demonstrate that ferruginol (1) and some phthalimide containing analogues 2-12 have potential antimalarial activity. The compounds were evaluated against malaria strains 3D7 and K1, and cytotoxicity was measured against a mammalian cell line panel. A promising lead, compound 3, showed potent activity with an EC50 = 86 nM (3D7 strain), 201 nM (K1 strain) and low cytotoxicity in mammalian cells (SI > 290). Some structure-activity relationships have been identified for the antimalarial activity in these abietane analogues. (C) 2014 Elsevier Ltd. All rights reserved.
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