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. Author manuscript; available in PMC: 2019 Jun 24.
Published in final edited form as: J Med Chem. 2019 Apr 18;62(9):4350–4369. doi: 10.1021/acs.jmedchem.8b01772

Table 1.

SRE.L Activity of 5-Aryl-1,3,4-Oxadiazole-2-thiopropionic acids

graphic file with name nihms-1036286-t0012.jpg
Cmpd R1 R2 R3 R4 SRE.L IC50 (nM)a, b
8a H H H H 3,500
8b H H Cl H 340
8c H H Me H 34
8d H H OMe H 160
8e H Cl H H 1,500
1 H Me H H 180
8f H OMe H H 3,600
8g Cl H H H 25
8h Me H H H 6,300
8i OMe H H H 3,100
8j Cl H Cl H 4 (2c)
8k Cl H Me H 1.5
8l Cl H OMe H 2.6
8m Cl Me Me H 0.02c
8n Cl H Me Me 0.23c
8o Cl H Cl Me 0.32c
a

Inhibition of Gα12-stimulated SRE.L activity (mean of n = 3, SEM < 10%) in PC3 cells unless otherwise noted.

b

Cell viability and proliferation assay with WST-1 < 5% inhibition up to 100 μM inhibitor (mean of n = 3, SEM < 10%).

c

SRE.L assay performed in HEK293T cells (mean of n = 3, SEM < 10%).