Tetrac, a deaminated derivative of the thyroid hormome, has received some broad interest for
its ability to inhibit the spread of new blood vessels, i.e., angiogenesis. For an optimum activity, the action
of the dug shall be limited at the cell surface for interaction with the integrin alpha v beta 3. This
was shown to be achieved via a nanoparticle formulation that would be grafted to Tetrac phenol’s OH.
While the principle of this study has been disclosed elsewhere, the broad results have never been disclosed
entirely. Here all outcomes of the synthesis strategy, e.g., protection and activation steps, confirmed
Triisopropylsillyl as a protective group of choice to access the nanoparticle. Catalyst assisted
esterification has been probed and discussed. Then the HPLC-MS study allowed to clarify reaction conditions
that could subsequently yield to the desired activated Tetrac moiety. The reaction products were
all characterized by 1H and 13C-NMR.
Tetrac是一种甲状腺激素的去氨基衍生物,因其抑制新血管生长即血管生成的能力而受到广泛关注。为了获得最佳活性,该药物的作用应限制在细胞表面与整合素αvβ3相互作用。通过将纳米颗粒配方移植到Tetrac酚的OH上,已经证明可以实现这一点。虽然该研究的原则已在其他地方披露,但广泛的结果从未完全披露。这里介绍了合成策略的所有结果,例如保护和激活步骤,确认了三异丙基硅基作为访问纳米颗粒的保护基的选择。探讨了催化剂辅助酯化反应。然后,HPLC-MS研究使得可以澄清随后可以产生所需活性Tetrac基团的反应条件。所有反应产物均通过1H和13C-NMR进行了表征。