当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Abstract：

:New inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered using an N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series was found to be potent in a porcine TACE (pTACE) assay with IC(50)s typically below 5 nM. For most compounds, selectivity for pTACE relative to MMP-1,-2, and -9 is at least 300-fold. Compound 2o was potent in inhibition of TNFalpha production in a human whole blood assay (WBA) with an IC(50) of 0.42 micro M.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Duan JJ,Lu Z,Xue CB,He X,Seng JL,Roderick JJ,Wasserman ZR,Liu RQ,Covington MB,Magolda RL,Newton RC,Trzaskos JM,Decicco CP

doi

10.1016/s0960-894x(03)00313-5

subject

Has Abstract

pub_date

2003-06-16 00:00:00

pages

2035-40

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960894X03003135

journal_volume

13

pub_type

杂志文章

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