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

Abstract A series of aminoparthenolide analogs ( 6 – 37 ) were synthesized and evaluated for their anti-leukemic activity. Eight compounds exhibited good anti-leukemic activity with LD 50 ’s in the low μM range (1.5–3.0 μM). Compounds 16 , 24 and 30 were the most potent compounds in the series, causing greater than 90% cell death at 10 μM concentration against primary AML cells in culture, with LD 50 values of 1.7, 1.8 and 1.6 μM.