An improved synthesis of a selective alpha(v)beta(3)-integrin antagonist cyclo(-RGDfK-)

作者：Dai XD; Su Z; Liu JO^*

来源：Tetrahedron Letters, 2000, 41(33): 6295-6298.

DOI：10.1016/S0040-4039(00)01060-1

• alpha(v)beta(3)-integrin antagonist
• cyclic RGD peptide
• solid-phase synthesis

The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the alpha(v)beta(3) 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.

• 出版日期2000-8-12
• 单位MIT