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 alpha,beta-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 mu M, respectively. These two 1-analogues are promising lead compounds for further investigation.
ROSSELLI S, BRUNO M, MAGGIO A, BELLONE G, CHEN T H, BASTOW K F LEE K H (2007). Cytotoxic activity of some natural and synthetic kauranes. JOURNAL OF NATURAL PRODUCTS, 70(3), 347-352 [10.1021/np060504w].
Cytotoxic activity of some natural and synthetic kauranes
ROSSELLI, Sergio;BRUNO, Maurizio;MAGGIO, Antonella Maria;BELLONE, Gabriella;
2007-01-01
Abstract
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 alpha,beta-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 mu M, respectively. These two 1-analogues are promising lead compounds for further investigation.
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