Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
2007
Abstract A series of β-sulfonyl hydroxamate TACE inhibitors, bearing a butynylamino or a butynyloxy P1′ group, was designed and synthesized. Of the compounds investigated, 22 has excellent potency against isolated TACE enzyme, shows good selectivity over MMP-2 and MMP-13, and oral activity in an in vivo mouse model of TNF-α production.
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