Incorporation of thioether building blocks into an αvβ3‐specific RGD peptide: Synthesis and biological activity

摘要: We report the design, synthesis, and binding affinities of a family thioether analogues alpha(v)beta(3)-specific compound c[(Mpa)RGDD(tBuG)C]-NH(2). The synthesis building blocks is scalable produced desired products in good yields. linear peptides were synthesized on solid supports, followed by cyclization solution. Our demonstrate interesting data to isolated receptors. In particular, peptide c[NH-Arg-Gly-Asp-Asp-(tBuG)-Cys(S-CH(2)-CO)]NH(2) (1) exhibits differences when compared parent demonstrates potent affinity alpha(v)beta(3) alpha(5)beta(1) receptors while having reduced alpha(IIb)beta(3) receptor. This result combined with replacement disulfide makes this for further development.