Derivatives of purinic and pyrimidinic antiviral agents and use thereof as potent anticancer agents

摘要

Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.

主权项

1. A compound having Formula I: wherein: R1 is H; R2 is an acyl moiety selected from the group consisting of valproyl, 4-phenylbutyryl, cinnamoyl, 2-(4-isobutylphenyl)propionyl, 1-(butyryloxymethoxy)succinyl, 1-(valproyloxymethoxy)succinyl, 1-(4-phenylbutyryloxymethoxy)succinyl, 1-(cinnamoyloxymethoxy)succinyl, 1-(phenylacetoxymethoxy)succinyl and 1-(2-(4-isobutylphenyl)propionyloxymethoxy)succinyl; and R3 and R4 are each independently hydrogen or an acyl moiety selected from the group consisting of valproyl, 4-phenylbutyryl, cinnamoyl, 2-(4-isobutylphenyl)propionyl, 1-(butyryloxymethoxy)succinyl, 1-(valproyloxymethoxy)succinyl, 1-(4-phenylbutyryloxymethoxy)succinyl, 1-(cinnamoyloxymethoxy)succinyl, 1-(phenylacetoxymethoxy)succinyl and 1-(2-(4-isobutylphenyl)propionyloxymethoxy)succinyl.