Janeen Marsha Linsley

Squaric acid derivatives as VLA-4 integrin antagonists.

SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.

Discovery and evaluation of potent, cysteine-based α4β1 integrin antagonists

Abstract Acyclic, disulphide derivatives of cysteine have been identified as moderately potent antagonists of α4β1-mediated leukocyte cell adhesion to VCAM. This communication describes how they were discovered from a simple l -cystine derivative and using the structure–activity data of C*DThioPC* related cyclic peptides.