Disclosed are pyrimidyl guanidine derivatives having anticancer activity. The pyimidyl guanidine derivatives have the structure: R1 is a cyclic (1-7 member) or acyclic (1-7 member) aliphatic, aromatic, heterocyclic groups optionally substituted, R2 is a cyclic (3-7 member) aliphatic, aromatic, heterocyclic groups optionally substituted by functional groups and R3 is a cyclic (3-7 member) aliphatic, aromatic, heterocyclic groups.