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

C - Chemistry, Metallurgy

07

D

167/208, 260/304

C07D 493/00 (2006.01) A61K 31/42 (2006.01) C07D 493/18 (2006.01) C07F 9/547 (2006.01)

Patent

CA 1334757

Rhizoxin and rhizoxin-2-ene derivatives of formula (I): Image (I) [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 R1 and R2, where R1 and R2 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.

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