Antitumor Agents: LXXXVII. Cytotoxic Antileukemic Canthin-6-one Alkaloids fromBrucea antidysentericaand the Structure Activity Relationships of their Related Derivatives1
- 1 April 1987
- journal article
- research article
- Published by Georg Thieme Verlag KG in Planta Medica
- Vol. 53 (02) , 140-143
- https://doi.org/10.1055/s-2006-962656
Abstract
Two cytotoxic antileukemic alkaloids, 11-hydroxy-1-methoxycanthin-6-one (2) and 1-hydroxy-11-methoxycanthin-6-one (3), as well as 1-methoxycanthin-6-one (1) were isolated from Brucea antidysenterica. The methyl ether (7) and a series of esters (8-13) of 11-hydroxycanthin-6-one (5) were prepared for investigating the structure-activity relationships. The results indicated that 1,11-dimethoxycanthin-6-one (4) and 11-hydroxycanthin-6-one (5) showed the most potent cytotoxic activity. Hydroxylation or methoxylation of canthin-6-one alkaloids at C-11 or C-10 are the structural requirement for the potent cytotoxicity in the KB tissue culture cell. Hydroxylation or methoxylation at C-1 of these alkaloids has no significant effect upon cytotoxicity.Keywords
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