Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.

@article{Sulyok2001SolidphaseSO,
  title={Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.},
  author={G{\'a}bor A. G. Sulyok and Christoph Gibson and Simon L Goodman and G{\"u}nter H{\"o}lzemann and Markus Wiesner and Horst Kessler},
  journal={Journal of medicinal chemistry},
  year={2001},
  volume={44 12},
  pages={1938-50}
}
The solid-phase synthesis of a low molecular weight RGD mimetic library is described. Activities of the compounds in inhibiting the interaction of ligands, vitronectin and fibrinogen, with isolated immobilized integrins alphavbeta3 and alphaIIbbeta3 were determined in a screening assay. Highly active and selective nonpeptide alphavbeta3 integrin antagonists with regard to orally bioavailability were developed, based on the aza-glycine containing lead compound 1. An important variation is the… CONTINUE READING