An improved synthesis of a selective αvβ3-integrin antagonist cyclo(-RGDfK-)

X. Dai, Z. Su, J. O. Liu

Research output: Contribution to journalArticlepeer-review


The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the αvβ3 integrin. A related compound, cyclo(-Arg-Gly'Asp-D-Phe-Val-), is a promising anticancer drug candidate; it inhibits angiogenesis and induces apoptosis in vascular cells. We have developed an improved solid-phase synthesis based on Kessler's procedure to afford cyclo(-RGDfK-) peptide in high purity and high yield in a multi-gram scale. This improved synthesis is environmentally friendly and may be generally applicable to other related cyclic peptide syntheses. (C) 2000 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)6295-6298
Number of pages4
JournalTetrahedron Letters
Issue number33
StatePublished - Aug 12 2000
Externally publishedYes


  • Cyclic RGD peptide
  • Solid-phase synthesis
  • αvβ3-integrin antagonist

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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