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  • Title: Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
    Author: Duan JJ, Chen L, Wasserman ZR, Lu Z, Liu RQ, Covington MB, Qian M, Hardman KD, Magolda RL, Newton RC, Christ DD, Wexler RR, Decicco CP.
    Journal: J Med Chem; 2002 Nov 07; 45(23):4954-7. PubMed ID: 12408705.
    Abstract:
    New gamma-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.
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