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

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

doi:10.1016/j.bmcl.2003.10.045

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

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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 language	English
Pages (from-to)	421-425
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2003.10.045
State	Published - Jan 2004
Externally published	Yes

Keywords

Angiogenesis
Prodrug
Telomers
Thalidomide

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10.1016/j.bmcl.2003.10.045

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title = "Inhibition of angiogenesis by THAM-derived cotelomers endowed with thalidomide moieties",

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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AU - Périno, Sandrine

AU - Contino-Pépin, Christiane

AU - Satchi-Fainaro, Ronit

AU - Butterfield, Catherine

AU - Pucci, Bernard

PY - 2004/1

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AB - 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.

KW - Angiogenesis

KW - Prodrug

KW - Telomers

KW - Thalidomide

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JO - Bioorganic and Medicinal Chemistry Letters

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

Abstract

Keywords

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