Rhizoxin derivatives and their use as anti-tumor agents

Details Rhizoxin derivatives and their use as anti-tumor agents Rhizoxin derivatives and their use as anti-tumor agents

1994-02-14

1995-02-21

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548235, 548236, C07D49318

Patent

active

053915640

ABSTRACT:
Rhizoxin and rhizoxin-2-ene derivatives of formula (I): ##STR1## in which: n is 1 to 25: A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.

REFERENCES:
Burger, "Medicinal Chemistry 2d Ed.", Interscience, N.Y., 1960, p. 42.
Ueda et al., Chem. Abstr., vol. 113, entry 218230y abstracting Japan 02196789 (1990).
Kaneko et al., Chem. Abstr., vol. 113, entry 114948x abstracting Europe 350 315 (1990).

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