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. 2014 May 23;136(22):7877–7888. doi: 10.1021/ja502310r

Table 1. Design and Mdm2 Binding Properties of Preliminary Oxopiperazine-Derived Helix Mimetics.

graphic file with name ja-2014-02310r_0015.jpg

mimetic R1 R2 R3 R4 X Kd (μM)a
1 Phe Trp Ala Leu OH 65 ± 8
2 Phe Trp Lys Leu OH ≥200
3 Phe Trp Leu Leu OH 7.9 ± 0.5
4 Phe Trp Phe Leu OH 6.9 ± 1.3
5 Phe Trp Phe Leu NH2 2.9 ± 0.1
6 Phe Trp Phe Lys NH2 ≥200
7 Lys Trp Phe Leu NH2 ≥200
8 Phe Ala Phe Leu NH2 64 ± 7
a

Binding affinity for Mdm2 as determined by a competitive fluorescence polarization assay.