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Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.

Abstract：

:p38alpha Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38alpha kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-alpha). The central role of p38alpha activation in settings of both chronic and acute inflammation has led efforts to find inhibitors of this enzyme as possible therapies for diseases such as rheumatoid arthritis, where p38alpha activation is thought to play a causal role. Herein, we report structure-activity relationship studies on a series of indole-based heterocyclic inhibitors that led to the design and identification of a new class of p38alpha inhibitors.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Mavunkel BJ,Chakravarty S,Perumattam JJ,Luedtke GR,Liang X,Lim D,Xu YJ,Laney M,Liu DY,Schreiner GF,Lewicki JA,Dugar S

doi

10.1016/s0960-894x(03)00653-x

subject

Has Abstract

pub_date

2003-09-15 00:00:00

pages

3087-90

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960894X0300653X

journal_volume

13

pub_type

杂志文章

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