| Autor: |
Duan, J. J.-W., Chen, L., Wasserman, Z. R., Lu, Z., Liu, R.-Q., Covington, M. B., Qian, M., Hardman, K. D., Magolda, R. L., Newton, R. C., Christ, D. D., Wexler, R. R., Decicco, C. P. |
| Zdroj: |
Journal of Medicinal Chemistry; November 2002, Vol. 45 Issue: 23 p4954-4957, 4p |
| Abstrakt: |
New γ-lactam TACE inhibitors were designed from known MMP inhibitors. A homology model of TACE was built and examined to identify the S1 site as the key area for TACE selectivity over MMPs. Rational exploration of the P1−S1 interactions resulted in the discovery of the 3,5-disubstituted benzyl ether as a TACE-selective P1 group. Further optimization led to the discovery of IK682 as a selective and orally bioavailable TACE inhibitor. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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