347382-76-7

Upstream product

• 112766-18-4 methyl N-(tert-butoxycarbonyl)-O-[(trifluoromethyl)sulfonyl]-L-tyrosinate 
• 4326-36-7 (S)-N-(tert-butoxycarbonyl)tyrosine methyl ester 
• 1080-06-4 L-Tyr-OMe 
• 60-18-4 L-tyrosine 
• 347382-77-8 (L)-4-(2',6'-dimethoxyphenyl)-phenylalanine 
• 82911-69-1 N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide 
• 347382-68-7 N-(trans-4-carboxycyclohexane-1-carbonyl)-4-(2,6-dimethoxyphenyl)-L-phenylalanine 
• 232276-95-8 methyl (2S)-2-amino-3-[4-(2,6-dimethoxyphenyl)phenyl]propanoate monohydrochloride 

Relevant academic research and scientific papers

Synthesis and biological evaluation of tyrosine modified analogues of the α4β7 integrin inhibitor biotin-R8ERY

The α4β7 integrin is a well-known target for the development of drugs against various inflammatory disease states including inflammatory bowel disease, type 1 diabetes and multiple sclerosis. The synthesis of a small library of cell-permeable β7 integrin inhibitors based on the peptide biotin-R8ERY is reported, in which the tyrosine residue has been modified by using the Suzuki-Miyaura cross-coupling reaction. The synthesised peptidomimetics were evaluated in a cell adhesion assay and shown to inhibit Mn2+-activated adhesion of mouse TK-1 T cells to mouse MAdCAM-1. All of the synthesised peptidomimetics are more active than our previously reported lead compound biotin-R8ERY with two of the analogues, 6 and 7, exhibiting IC50 values of 15 μM.

New phenylalanine derivatives

Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to α4β7 integrin and a selectivity toward α4β1 integrin. They are used as therapeutic agents for various diseases to which α4β7 integrin relates.