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Among those, the tyrosine derivative 28 exhibited a Ki value of 4.1 nM and the corresponding analogue with a saturated double bond, compound 29 , a Ki value of 25 nM, demonstrating that a proper constrain of flexibility of the ring system, alternatively an electron density in the center of the lipophilic bridge between amino acid residues in positions 1 and 3 is favorable for affinity to IRAP (Figure 7)

Each batch is independently tested by Janoshik Analytical (Prague, Czech Republic) for HPLC purity, mass spectrometry confirmation, and copper content by atomic absorption spectroscopy

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