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Bioorg Med Chem Lett. 2009 Sep 15;19(18):5321-4. doi: 10.1016/j.bmcl.2009.07.151. Epub 2009 Aug 3.

Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.

Author information

1
Boehringer Ingelheim Pharmaceuticals, Department of Medicinal Chemistry, 900 Ridgebury Rd, Ridgefield, CT 06877, USA. alexander.heim-riether@boehringer-ingelheim.com

Abstract

Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode distinct from previously published MMP-13 inhibitors. Potency and selectivity were improved by extending the hit structure out from the active site into the S1' pocket.

PMID:
19692239
DOI:
10.1016/j.bmcl.2009.07.151
[Indexed for MEDLINE]

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