5'-DEOXYCYTIDINE DERIVATIVES

摘要

Compounds of general formula (I) wherein R1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions; R2 is -(CH2)n-cycloalkyl (wherein cycloalkyl consists of 3 to 5 carbon atoms, n is an integer from 0 to 4), heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), araykylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino) (lower-alkyl) wherein the alkylene chain may be further substituted with one or two lower-alkyl group(s) and R3 is iodo, a vinyl or ethynyl group ¢which groups may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or an aromatic ring which may have one or more hetero atom(s)!, are useful in the treatment of malignant diseases and can also be administered together with 5-fluorouracil or derivatives thereof to enhance the antitumour activity of the latter.