Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs

摘要

An angiogenesis-inhibiting compound is described to be used for the manufacture of a composition for the treatment of undesired angiogenesis in a human or animal. The undesired angiogenesis is disclosed to be associated with diseases such as retinal/choroidal neovascularization, corneal neovascularization, retinopathy of prematurity, or neovascular glaucoma. The compound comprises the formula A, B, or C, or combinations thereof, wherein: R1 is independently -H, -OH, -CH3, -CH2OZ, -CH2OCONZ, or -CH2Z, wherein Z is H or -(CH2)n-H, where n is 1-10; R2 is independently selected from -NH-NH2, -NH-OH, -NH-OR3, -N=N-R3, -N(R3)2, -NHCOH, -NHCOCH3, pyrazolidine, or imidazoline; and R3- is independently selected from pyrazolidine, pyrazoline, tetrazole, imidazole, pyrazole, piprazine, or imidazoline.