Rhizoxin derivatives and their use as anti-tumor agents
AssigneeSankyo Company, Limited
InventorsMasakatsu Kaneko, Makoto Kamokari, Tomowo Kobayashi, Kazuhiko Sasagawa
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AssigneeSankyo Company, Limited
InventorsMasakatsu Kaneko, Makoto Kamokari, Tomowo Kobayashi, Kazuhiko Sasagawa
Estimating the term…
Rhizoxin and rhizoxin-2-ene derivatives of formula ##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.
A compound of the formula (I):
The compound of claim 1, wherein X represents NR and R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen atoms;
Rhizoxin-13-yl 12-hydroxydodecanoate and pharmaceutically acceptable salts and esters thereof.
Rhizoxin-13-yl 12-propionyloxydodecanoate and pharmaceutically acceptable salts and esters thereof.
Rhizoxin-13-yl 12-valeryloxydodecanoate and pharmaceutically acceptable salts and esters thereof.
Dependencies are inferred from the claim text.