Antileukemic trichotecene epoxides

Details Antileukemic trichotecene epoxides Antileukemic trichotecene epoxides

C - Chemistry, Metallurgy

07

D

260/350.7

C07D 493/22 (2006.01) C07D 493/20 (2006.01)

Patent

CA 1123443

ABSTRACT OF THE DISCLOSURE There are provided novel anti-leukemic epoxides which are isolated from Baccharis megapotamica. The novel compounds are characterized by a 12, 13- epoxytrichothecene central ring system which is spanned by a dienic macrolide ester side chain. The active compounds are characterized by the presence of an oxygen atom in the A-ring which takes the form of either a beta hydroxy group in the 8 position together with an unsaturated bond at the 9: 10 position or, alternatively, an epoxide group lying between the 9 and 10 position. Compounds devoid of either of these groups show no anti-leukemic activity. The active compounds possess high and surprising anti-leukemic activity against P-388 lymphocytic leukemia in in vivo assays in mice. The invention described herein was made in the course of work under grants or awards from the Department of Health, Education and Welfare.

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