Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13)

被引:92
作者
Kim, SH [1 ]
Pudzianowski, AT [1 ]
Leavitt, KJ [1 ]
Barbosa, J [1 ]
McDonnell, PA [1 ]
Metzler, WJ [1 ]
Rankin, BM [1 ]
Liu, R [1 ]
Vaccaro, W [1 ]
Pitts, W [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Princeton, NJ 08560 USA
关键词
MMP-13; inhibition; barbituric acid; structure-based design;
D O I
10.1016/j.bmcl.2004.12.016
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Computer aided drug design led to a new class of spiro-barbiturates (e.g., 4a, MMP-13 K-i = 4.7 nM) that are potent inhibitors of MMP-13. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1101 / 1106
页数:6
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