Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties

Sandrine Périno, Christiane Contino-Pépin*, Ronit Satchi-Fainaro, Catherine Butterfield, Bernard Pucci

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

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.

Original languageEnglish
Pages (from-to)421-425
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number2
DOIs
StatePublished - Jan 2004
Externally publishedYes

Keywords

  • Angiogenesis
  • Prodrug
  • Telomers
  • Thalidomide

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