ORBi: Kempen I. - 6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of the Treatment of Cancer Cell Invasion and Metastasis

Reference : 6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of t...


	Document type :	Scientific journals : Article
	Discipline(s) :	Life sciences : Biochemistry, biophysics & molecular biology
	To cite this reference:	http://hdl.handle.net/2268/9663

Title :	6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of the Treatment of Cancer Cell Invasion and Metastasis
Language :	English
Author, co-author :	Kempen, I. [> > > >]
	Hemmer, Marc [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
	Counerotte, Stéphane [Université de Liège - ULg > > Chimie pharmaceutique >]
	Pochet, L. [> > > >]
	De Tullio, Pascal [Université de Liège - ULg > > Chimie pharmaceutique >]
	Foidart, Jean-Michel [Université de Liège - ULg > Département des sciences cliniques > Gynécologie - Obstétrique >]
	Blacher, Silvia [Université de Liège - ULg > Département des sciences cliniques > Labo de biologie des tumeurs et du développement >]
	Noël, Agnès [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Biologie cellulaire et moléculaire appliquée à l'homme >]
	Frankenne, Francis [ > > ]
	Pirotte, Bernard [Université de Liège - ULg > > Chimie pharmaceutique >]
Publication date :	Dec-2008
Journal title :	European Journal of Medicinal Chemistry
Publisher :	Elsevier
Volume :	43
Issue/season :	12
Pages :	2735-50
Audience :	International
ISSN :	0223-5234
City :	Paris
Country :	France
Keywords :	[en] Coumarin derivatives ; Cancer ; Cell invasion ; Anti-cancer
Abstract :	[en] Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated. Structure-activity relationships were deduced from biological results and will be used in further design of new active compounds. In particular, the acetoxymethyl substituent found at the 6-position of previously described active compounds can be replaced by an acetamidomethyl substituent without loss of potency; while the presence of an aryl ester function at the 3-position was preferred to a thioester or an amide function to induce marked biological activity. This work confirms the interest of aryl esters of 6-substituted coumarin-3-carboxylic acids as potential new anti-cancer agents.
Permalink :	http://hdl.handle.net/2268/9663
DOI :	10.1016/j.ejmech.2008.01.024

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