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

作者：Neelakantan Sundar; Nasim Shama; Guzman Monica L; Jordan Craig T; Crooks Peter A^*

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(15): 4346-4349.

DOI：10.1016/j.bmcl.2009.05.092

• Sesquiterpene lactone
• Parthenolide
• Aminoparthenolide analogs
• NF-kappa B inhibitor
• DMAPT (LC-1)
• Anti-leukemic activity
• Leukemia

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 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 LD(50) values of 1.7, 1.8 and 1.6 mu M.

• 出版日期2009-8-1