Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-κB inhibitor, DMAPT (LC-1)
Graphical abstract
A series of water-soluble parthenolide (1) analogs (6–37) were synthesized and evaluated for anti-leukemic activity against primary acute myelogenous (AML) cells in culture. Analogs 16 (R1 = R2 = CH3), 24 (R1 = CH3, R2 = CH2CH2OH) and 30 (R1, R2 = (CH2)2CH(CH3)(CH2)2 had LD50 values in the range 1.6–1.8 μM.
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Acknowledgement
This work was supported by a grant from the Kentucky Lung Cancer Research Program.
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