Anti-leukemic trichothecene epoxides

Drug – bio-affecting and body treating compositions – Nonspecific immunoeffector – per se ; or nonspecific... – Synthetic or structurally-modified peptidoglycan or...

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26034341, C07D49322, A61K 31365

Patent

active

041645847

ABSTRACT:
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.

REFERENCES:
moreira et al., Chem. Absts., 8816f, vol. 66, 1967.
Montes et al., Chem. Absts., vol. 75, 1971, 115887k.
Kupchan et al., Chem. Absts., 31262q, vol. 75, 1971.
Dominguez et al., Chem. Absts., 98760k, vol. 77, 1972.

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