In the angiogenesis process, integrins, which are members of a family of cell surface transmembrane receptors, play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as l-thyroxine (T₄) and 3,5,3′-triiodo-l-thyronine (T₃) promote angiogenesis and tumor cell proliferation via integrin αvβ3 receptor. At or near an arginine-glycine-aspartate (RGD) recognition site on the binding pocket of integrin α_vβ₃, tetraiodothyroacetic acid (tetrac, a deaminated derivative of T₄) is a thyrointegrin receptor antagonist and blocks the actions of T₃ and T₄ as well as different growth factors-mediated angiogenesis. In this study, we synthesized novel tetrac analogs by modifying the phenolic moiety of tetrac and tested them for their anti-angiogenesis activity using a Matrigel plug model for angiogenesis in mice. Pharmacological activity results showed that tetrac can accommodate numerous modifications and maintain its anti-angiogenesis activity.

在血管生成过程中，整联蛋白是细胞表面跨膜受体家族的成员，在血管形成和血管生长因子的局部释放中起着至关重要的作用。甲状腺激素，例如升-thyroxine（T ₄）和3,5,3'-三碘-升-甲腺氨酸（T ₃），通过整合素αvβ3受体促进血管发生和肿瘤细胞增殖。处或附近的精氨酸-甘氨酸-天门冬氨酸上的整合素α结合口袋（RGD）的识别位点_v β ₃，tetraiodothyroacetic酸（tetrac，T的脱氨基衍生物₄）是thyrointegrin受体拮抗剂和块T的动作₃和第₄以及不同的生长因子介导的血管生成。在这项研究中，我们通过修饰tetrac的酚部分合成了新颖的tetrac类似物，并使用用于小鼠血管生成的Matrigel栓塞模型测试了它们的抗血管生成活性。药理活性结果表明，tetrac可以适应多种修饰并保持其抗血管生成活性。