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. Author manuscript; available in PMC: 2022 Jul 5.
Published in final edited form as: Eur J Med Chem. 2021 Apr 4;219:113425. doi: 10.1016/j.ejmech.2021.113425

Table 1.

Evaluation of cell growth inhibition of the synthesized MDM2 degraders in RS4;11 leukemia cells

graphic file with name nihms-1690864-t0015.jpg
Cmp. No R1 R2 n IC50 (nM)a
1b 3,4,5-trifluoro COOEt - 2700
3 H COOEt 2 56
4 H COOEt 3 7.6
5 H COOEt 4 4.8
6 4-Cl COOEt 2 1403
7 4-Cl COOEt 3 5.3
8 4-Cl COOEt 4 1.3
9 3,4,5-trifluoro COOEt 2 95.9
10 3,4,5-trifluoro COOEt 3 3.2
11 (WB214) 3,4,5-trifluoro COOEt 4 1.2
12 3,4,5-trifluoro COOEt 5 0.76
13 3,4,5-trifluoro COOEt 6 2.6
14 3,4,5-trifluoro COOEt 7 3.0
15 3,4,5-trifluoro COOEt 8 250
16 3,4,5-trifluoro COOH 4 >10 μM
17 3,4,5-trifluoro CONHEt 4 2.4
a.

The cell growth inhibition (IC50) of the compounds were measured in RS4;11 leukemia cells by Alarma Blue assay.

b.

The reported data of the cell growth inhibition (IC50) of Ugi ligand 1 in SJSA-1 cells by MTT assay.