Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-κB inhibitor, DMAPT (LC-1)

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.