Discovery of a new class of p38 kinase inhibitors

  • Bioorg Med Chem Lett. 2000 Sep 18;10(18):2047-50. doi: 10.1016/s0960-894x(00)00270-5.
J Dumas  1 ,  R Sibley ,  B Riedl ,  M K Monahan ,  W Lee ,  T B Lowinger ,  A M Redman ,  J S Johnson ,  J Kingery-Wood ,  W J Scott ,  R A Smith ,  M Bobko ,  R Schoenleber ,  G E Ranges ,  T J Housley ,  A Bhargava ,  S M Wilhelm ,  A Shrikhande
Affiliations
  • 1. Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA. [email protected]
PMID: 10999467 DOI: 10.1016/s0960-894x(00)00270-5
Abstract

The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure-activity relationships are observed within this class.