Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.

Abstract:

:The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.

journal_name

Bioorg Med Chem Lett

authors

Levin JI,Chen JM,Laakso LM,Du M,Du X,Venkatesan AM,Sandanayaka V,Zask A,Xu J,Xu W,Zhang Y,Skotnicki JS

doi

10.1016/j.bmcl.2005.06.072

subject

Has Abstract

pub_date

2005-10-01 00:00:00

pages

4345-9

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00803-6

journal_volume

15

pub_type

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