Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 18, Pages 5464-5472Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.07.036
Keywords
Haemanthamine; Antiplasmodial activity; Amaryllidaceae alkaloids
Funding
- Spanish MICINN [SAF 2009-13296-C02-01]
- ICIC (Instituto Canario de Investigacion del Cancer)
- Gobierno Autonomo de Canarias
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Thirty one derivatives were prepared from the natural alkaloids haemanthamine (1), haemanthidine (2) and 11-hydroxyvittatine (3). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum and some structure-activity relationships were outlined. For haemanthamine derivatives having a methoxy group at C-3, the presence of a free hydroxyl group at C-11 is important for the activity. The double bond at C-1-C-2 plays also an important role to achieve good inhibitory activity. Compound 35 with two nicotinate groups at C-3 and at C-11 was the most active compound with a IC50 = 0.8 +/- 0.06 mu M. (C) 2012 Elsevier Ltd. All rights reserved.
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