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Published on: May 15, 2019
Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties
Sandrine Périno1, Christiane Contino-Pépin, Ronit Satchi-Fainaro
1Laboratoire de Chimie Bioorganique et des Systèmes Moléculaires Vectoriels, Faculté des Sciences, 33, rue Louis Pasteur, 84000, Avignon, France.
Abstract:
The synthesis of a tris(hydroxymethyl)acrylamidomethane (THAM)-derived cotelomer endowed with thalidomide units and a preliminary assessment of its biological activity are described. 4-Carboxy thalidomide and 4-(N-acryloyl) lysine thalidomide derivatives were prepared. The polymerization of these compounds with THAM in the presence of octanethiol as transfer reagent provided a water-soluble telomer bearing several thalidomide units. The ability of this telomer to inhibit angiogenesis in a mouse model of corneal neovascularization was compared to 4-carboxy thalidomide and thalidomide. A significant inhibition in area of neovascularization stimulated by a bFGF pellet was observed only in the mice treated with the telomer.
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