6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives in a new approach of the treatment of cancer cell invasion and metastasis

被引:53
作者
Kempen, Isabelle [1 ]
Hemmer, Marc [1 ]
Counerotte, Stephane [1 ]
Pochet, Lionel [2 ]
de Tullio, Pascal [1 ]
Foidart, Jean-Michel [3 ]
Blacher, Silvia [3 ]
Noel, Agnes [3 ]
Frankenne, Francis [3 ]
Pirotte, Bernard [1 ]
机构
[1] Univ Liege, Lab Chim Pharmaceut, Drug Res Ctr, B-4000 Liege, Belgium
[2] Univ Namur, Dept Pharm, FUNDP, B-5000 Namur, Belgium
[3] Univ Liege, Lab Biol Tumeurs & Dev, B-4000 Liege, Belgium
关键词
Coumarin derivatives; Cancer; Cell invasion; Anti-cancer drug;
D O I
10.1016/j.ejmech.2008.01.024
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2008 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:2735 / 2750
页数:16
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