Abstract
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 language | English (US) |
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Pages (from-to) | 6295-6298 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 41 |
Issue number | 33 |
DOIs | |
State | Published - Aug 12 2000 |
Externally published | Yes |
Keywords
- Cyclic RGD peptide
- Solid-phase synthesis
- αvβ3-integrin antagonist
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry