Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5218173 | Tetrahedron | 2012 | 8 Pages |
Abstract
A scalable, solution-phase synthesis of the selectively protected non-peptide RGD (arginine-glycine-aspartic acid) mimetic 6 is described. This synthesis serves as an alternative to the previously described solid-phase synthesis of this compound, thereby making this important integrin-binding mimetic readily accessible. The free carboxylic acid of 6 was conjugated to a protected diamine, followed by global deprotection to give a derivative 27, suitable for immobilization onto amine-reactive surfaces. The RGD mimetic 28 demonstrated superior biological activity in comparison to a native linear RGD peptide and the semi-synthetic cyclic cRGDfK peptide in a cell attachment inhibition assay.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Andrew G. Riches, Teresa Cablewski, Veronica Glattauer, Helmut Thissen, Laurence Meagher,