Structural requirements for biological activity among antileukemic glaucarubolone ester quassinoids

Abstract

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 activiy. 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 [human oral carcinoma] KB cells in tissue cluture and inhibitory activity against the P-388 lymphocytic leukemia in mice.