| Literature DB >> 19410464 |
Kaapjoo Park1, Ariamala Gopalsamy, Alexis Aplasca, John W Ellingboe, Weixin Xu, Yuhua Zhang, Jeremy I Levin.
Abstract
A novel series of non-hydroxamate tryptophan sulfonamide derivatives containing a butynyloxy P1' moiety was identified as inhibitors of TNF-alpha converting enzyme (TACE). The structure-activity relationship of the series was examined via substitution on the tryptophan indole ring. Of the compounds investigated, 2-(4-(but-2-ynyloxy)phenylsulfonamido)-3-(1-(4-methoxybenzyl)-1H-indol-3-yl)propanoic acid (12p) has the best in vitro potency against isolated TACE enzyme with an IC(50) of 80 nM. Compound 12p also shows good selectivity over MMP-1, -13, -14.Entities:
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Year: 2009 PMID： 19410464 DOI： 10.1016/j.bmc.2009.04.033
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641