Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
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DOI：
10.1016/s0960-894x(00)00720-4
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发表时间：
2001-02
影响因子：
2.7
通讯作者：
M. Fray;R. Dickinson
中科院分区：
文献类型：
--
作者：
M. Fray;R. Dickinson
Structure–activity relationships are described for a series of succinyl hydroxamic acids 4a–o as potent and selective inhibitors of matrix metalloprotease-3 (stromelysin-1). Optimisation of P1′ and P3′ groups gave compound 4j (MMP-3 IC50=5.9nM) which was >140-fold less potent against MMP-1 (IC50=51,000nM), MMP-2 (IC50=1790nM), MMP-9 (IC50=840nM) and MMP-14 (IC50=1900nM).
