Article (Scientific journals)
6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of the Treatment of Cancer Cell Invasion and Metastasis
Kempen, I.; Hemmer, Marc; Counerotte, Stéphane et al.
2008In European Journal of Medicinal Chemistry, 43 (12), p. 2735-50
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Keywords :
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.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Kempen, I.
Hemmer, Marc ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Counerotte, Stéphane ;  Université de Liège - ULiège > Chimie pharmaceutique
Pochet, L.
De Tullio, Pascal ;  Université de Liège - ULiège > Chimie pharmaceutique
Foidart, Jean-Michel ;  Université de Liège - ULiège > Département des sciences cliniques > Gynécologie - Obstétrique
Blacher, Silvia ;  Université de Liège - ULiège > Département des sciences cliniques > Labo de biologie des tumeurs et du développement
Noël, Agnès ;  Université de Liège - ULiège > Département des sciences biomédicales et précliniques > Biologie cellulaire et moléculaire appliquée à l'homme
Frankenne, Francis
Pirotte, Bernard ;  Université de Liège - ULiège > Chimie pharmaceutique
Language :
English
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
Publication date :
December 2008
Journal title :
European Journal of Medicinal Chemistry
ISSN :
0223-5234
eISSN :
1768-3254
Publisher :
Elsevier, Paris, France
Volume :
43
Issue :
12
Pages :
2735-50
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 25 March 2009

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