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Cytotoxic Activity of Some Natural and Synthetic ent -Kauranes

2007; American Chemical Society; Volume: 70; Issue: 3 Linguagem: Inglês

10.1021/np060504w

1520-6025

Sergio Rosselli, Maurizio Bruno, Antonella Maggio, Gabriella Bellone, Tzu-Hsuan Chen, Kenneth F. Bastow, Kuo‐Hsiung Lee,

Phytochemical compounds biological activities

Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an α,β-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity against all six tested cancer cell lines and were most potent against 1A9 ovarian cancer cells with EC50 values of 0.2 and 0.3 μM, respectively. These two 1-analogues are promising lead compounds for further investigation.