کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375914 | 981947 | 2009 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors](/preview/png/1375914.png)
We have discovered nanomolar inhibitors of TNF-α convertase (TACE) comprised of a novel spirocyclic scaffold and either a carboxylate or hydroxamate zinc binding moiety. X-ray crystal structures and computer models of selected compounds binding to TACE explain the observed SAR. We report the first TACE X-ray crystal structure for an inhibitor with a carboxylate zinc ligand.
A novel class of TACE inhibitors having nanomolar potency is described. The compounds have a spirocyclic scaffold and either a carboxylate or hydroxamate zinc binding moiety. We report the first X-ray crystal structure for a TACE inhibitor with a carboxylate Zn ligand.The compounds have a spirocyclic scaffold and either a carboxylate or hydroxamate zinc binding moiety. We report the first X-ray crystal structure for a TACE inhibitor with a carboxylate Zn ligand.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 1, 1 January 2009, Pages 54–57