2. Academic Validation
  3. De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold

De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold

  • Bioorg Med Chem Lett. 2005 Feb 15;15(4):1161-4. doi: 10.1016/j.bmcl.2004.12.007.
Dominique Potin 1,  Michele Launay,  Eric Nicolai,  Maud Fabreguette,  Patrice Malabre,  François Caussade,  Dominique Besse,  Stacey Skala,  Dawn K Stetsko,  Gordon Todderud,  Brett R Beno,  Daniel L Cheney,  Chiehying J Chang,  Steven Sheriff,  Diane L Hollenbaugh,  Joel C Barrish,  Edwin J Iwanowicz,  Suzanne J Suchard,  T G Murali Dhar
Affiliations

Affiliation

  • 1 Cerep, 128, rue Danton, 92500 Rueil-Malmaison, France.
PMID: 15686933 DOI: 10.1016/j.bmcl.2004.12.007
Abstract

LFA-1 (leukocyte function-associated antigen-1), is a member of the beta(2)-integrin family and is expressed on all leukocytes. The LFA-1/ICAM interaction promotes tight adhesion between activated leukocytes and the endothelium, as well as between T cells and antigen-presenting cells. Evidence from both animal models and clinical trials provides support for LFA-1 as a target in several different inflammatory diseases. This paper describes the de novo design, synthesis and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.

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