Table 2.
IC50 values of the cyclic peptides as determined by cell adhesion assays with WM115 cells.
| Compound | IC50 [μM] [a] |
|---|---|
| cyclo-(-Arg-Gly-Asp-d-Phe-Val-) (1b) | 5.1 ± 1.8 |
| cyclo-[-Arg-Gly-Asp-(1S,2R)-β-ACPC-Val-] (8) | 75 ± 32.5 |
| cyclo-[-Arg-Gly-Asp-(1R,2S)-β-ACPC-Val-] (9) | 124.5 ± 10.6 |
| cyclo-[-isoAsp-Gly-Arg-(1R,2S)-β-ACPC-Val-] (10) | >300 |
[a] IC50 values were calculated as the concentration of compound required for 50% inhibition of cell adhesion to vitronectin. Cell adhesion assays were performed by incubating the immobilized vitronectin with fluorescein labeled cells and increasing concentrations (10−7–10−4 M) of the RGD and isoDGR ligands, and measuring the fluorescence of bound cells. All values are the arithmetic mean ± the standard deviation (SD) of two independent assays each with four replicate determinations.