N-SUBSTITUTED PHTHALIMIDE DERIVATIVES AS POTENTIAL ANGIOGENESIS INHIBITORS

摘要

The present invention relates to N- substituted phthalimide derivatives as potential angiogenesis inhibitors.. More particularly the analogues in which phthalimide moiety linked with phenyl or heterocyclic ring of benzothiazole and benzothiadiazole and having the general structure 1 : R1 is selected from the group consisting of H, halo, alkyl, alkoxy, amine and nitro; R2 is selected from the group consisting of non-substituted, substituted benzothiazole, benzoimidazole and benzothiadiazole and R3 is selected from the group consisting of H, halo, alkyl, alkoxy, amine and nitro. Three analogues were disclosed to have more potent anti-angiogenesis activity than thalidomide. These new N-benzothiazole substituted phthalimide analogues have therapeutic potential where angiogenesis need to be controlled, for example, these analogues can be used in broad spectrum of cancer related diseases alone, or in combination with existing therapies. The compounds can also be useful for the treatment of autoimmune diseases and inflammatory diseases like ENL. R1 = H, halo, alkyl, hydroxy, alkoxy, amine and nitro R3 = H, halo, alkyl, hydroxy, alkoxy, amine and nitro