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Updated: Aug 18, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
[Search for new anti-angiogenic agents with structural analogy with thalidomide]
1Laboratoire de chimie organique, UFR des sciences pharmaceutiques et biologiques, 4, avenue de l'Observatoire, F75270 Paris Cedex 06, France.
Abstract:
Despite its teratogenic effects, thalidomide has been reintroduced in human anticancer treatment for its anti-angiogenic activity, especially observed in patients with multiple myeloma. Here, we report the synthesis of new analogues designed to increase the thalidomide anti-tumour properties. The anti-angiogenic activity of the compounds was tested on EA.hy 926 endothelial cell lines. In this model, that is easier to manipulate than HUVEC cells, thalidomide is active in a similar dose range as reported on HUVEC cells and one of our compounds is more efficient.
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