Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 15, Pages 4346-4349Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.092
Keywords
Sesquiterpene lactone; Parthenolide; Aminoparthenolide analogs; NF-kappa B inhibitor; DMAPT (LC-1); Anti-leukemic activity; Leukemia
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Funding
- Kentucky Lung Cancer Research Program
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A series of aminoparthenolide analogs (6-37) were synthesized and evaluated for their anti-leukemic activity. Eight compounds exhibited good anti-leukemic activity with LD50's in the low mu M range (1.5-3.0 mu M). Compounds 16, 24 and 30 were the most potent compounds in the series, causing greater than 90% cell death at 10 mu M concentration against primary AML cells in culture, with LD50 values of 1.7, 1.8 and 1.6 mu M. (C) 2009 Elsevier Ltd. All rights reserved.
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