Highly Selective and Orally Active Inhibitors of Type IV Collagenase (MMP-9 and MMP-2): N-Sulfonylamino Acid Derivatives

Citations Over TimeTop 10% of 1998 papers

Abstract

Various N-sulfonylamino acid derivatives were synthesized and evaluated for their in vitro and in vivo activities to inhibit type IV collagenase (MMP-9 and MMP-2). When the amino acid residue and the sulfonamide moiety were modified, their inhibitory activities were greatly affected by the structure of the sulfonamide moiety. A series of aryl sulfonamide derivatives containing biaryl, tetrazole, amide, and triple bond were found to be potent and highly selective inhibitors of MMP-9 and MMP-2. In addition, these compounds were orally active in animal models of tumor growth and metastasis. These results revealed the potential of the N-sulfonylamino acid derivatives as a new type of candidate drug for the treatment of cancer.

Related Papers

• → Design and Synthesis of Phosphinamide-Based Hydroxamic Acids as Inhibitors of Matrix Metalloproteinases(1998)84 cited
• → The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors(1999)22 cited
• → A quantitative structure–activity relationship study on some series of anthranilic acid-based matrix metalloproteinase inhibitors(2005)21 cited
• → A quantitative structure-activity relationship study on matrix metalloproteinase inhibitors: Piperidine sulfonamide aryl hydroxamic acid analogs(2007)8 cited
• → A Quantitative Structure-Activity Relationship Study on a Novel Series of Hydroxamic Acid Analogs Acting as Matrix Metalloproteinase Inhibitors(2008)3 cited