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A C-15 ester substituent is required for significant antileukemic activity among the glaucarubolone ester quassinoids, and variations in the ester group are not accompanied by particularly marked changes in antileukemic activity. Unsaturation at the 3,4 position is advantageous for optimal activity, and hydrogenation of this double bond results in marked diminution in both cytotoxicity toward KB cells in tissue culture and inhibitory activity against the P-388 lymphocytic leukemia in mice.

Die Isolierung und Strukturau?dämng der antileukämisch wirksamen Substanzen Bruceantin (Ia) und Bruceantinol (Ic) sowie weiterer Quassinoide Bruceantarin (Ib), Dehydrobruceantin (IIa), Dehydrobruceantorin (IIb), Dehydrobrucein B (Ilc), Dehydrobruceantol (IId) sowie Isobrucein B (III) werden beschrieben.

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