1042927-01-4Relevant academic research and scientific papers
META-SUBSTITUTED PHENYL SULFONYL AMIDES OF SECONDARY AMINO ACID AMIDES, THE PRODUCTION THEREOF, AND USE THEREOF AS MATRIPTASE INHIBITORS
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Page/Page column 8, (2010/12/29)
The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors
Steinmetzer, Torsten,Doennecke, Daniel,Korsonewski, Martin,Neuwirth, Claudia,Steinmetzer, Peter,Schulze, Alexander,Saupe, Sebastian Martin,Schweinitz, Andrea
scheme or table, p. 67 - 73 (2009/04/16)
Replacement of the N-terminal β-alanyl-amide moiety in previously identified matriptase inhibitors by non-charged aryl groups caused a slightly decreased potency and partially reduced selectivity, especially towards thrombin. However, some of these analogues are still potent matriptase inhibitors with Ki-values i-value of 80 pM.
