A novel series of highly selective inhibitors of MMP-3
A novel series of highly selective inhibitors of MMP-3
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DOI：
10.1016/j.bmcl.2007.10.042
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发表时间：
2007-12-15
影响因子：
2.7
通讯作者：
Lewis, Mark L.
中科院分区：
文献类型：
--
作者：
Whitlock, Gavin A.;Dack, Kevin N.;Lewis, Mark L.
The design and synthesis of a series of highly selective hydroxamate inhibitors of stromelysin-1 (MMP-3) is described. Substitution of a 4-biaryl piperidine sulfonamide core, which binds at the S1' subsite of MMP-3, was optimised to give potent inhibitors of MMP-3, with greater than 300-fold selectivity over MMP-1, MMP-2, MMP-9 and MMP-14. Compounds 26 and 27 were identified as having the best balance of pharmacology and properties required for topical drug delivery. (c) 2007 Elsevier Ltd. All rights reserved.
