Synthesis of new analogs of tetraiodothyroacetic acid (tetrac) as novel angiogenesis inhibitors for treatment of cancer
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Date
2018-02-24
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Pergamon-Elsevier Science
Abstract
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 (T-4) and 3,5,30-triiodo-L-thyronine (T-3) promote angiogenesis and tumor cell proliferation via integrin alpha v beta 3 receptor. At or near an arginine-glycine-aspartate (RGD) recognition site on the binding pocket of integrin avb3, tetraiodothyroacetic acid (tetrac, a deaminated derivative of T-4) is a thyrointegrin receptor antagonist and blocks the actions of T-3 and T-4 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.
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Keywords
Pharmacology & pharmacy, Chemistry, Angiogenesis, Thyroid hormones, Tetraiodothyroacetic acid, Tetrac, Integrin, L-thyeoxine, Tumor, Thalidomide, Growth, Metabolites, Integrins
Citation
Rajabi, M. vd. (2018). ''Synthesis of new analogs of tetraiodothyroacetic acid (tetrac) as novel angiogenesis inhibitors for treatment of cancer''. Bioorganic and Medicinal Chemistry Letters, 28(7), 1223-1227.