Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) |
| |
| Authors: | Sawa Masaaki Kurokawa Kiriko Inoue Yoshimasa Kondo Hirosato Yoshino Kohichiro |
| |
| Affiliation: | Department of Chemistry, R&D Laboratories, Nippon Organon K.K., 1-5-90, Tomobuchi-cho, Miyakojima-ku, 16, Osaka 534-00, Japan. masaaki-sawa@dainippon-pharm.co.jp |
| |
| Abstract: | A novel series of phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
