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. Author manuscript; available in PMC: 2016 Mar 1.
Published in final edited form as: Bioorg Med Chem. 2015 Jan 13;23(5):1027–1043. doi: 10.1016/j.bmc.2015.01.011

Table 2.

Activity and cytotoxicity of T3SS inhibitors with varying substituents on the phenoxide ring.

graphic file with name nihms660087t2.jpg
Compound
#
X R R’ secretion
IC50 (µM)
translocation
IC50 (µM)
translocation
CC50 (µM)
1 CH −Cl −Cl 7.8 ± 2.0 11 ± 2 >100
12a CH −H −Cl 27.0 +/−4.2 >100 >100
12b CH −Cl −H 70.1 +/−0.7 >65 65.0 +/−4.2
12c CH −F −Cl 34 ± 1 >100 >100
12d CH −Cl −F >100 n.d. n.d.
12e CH −F −F >100 n.d. n.d.
12f CH −Me −Cl 34.0 +/−4.4 >100 >100
12g CH −CN −Cl >100 n.d. n.d.
12h CH −OMe −Cl >100 n.d. n.d.
16 N −Cl −Cl 5.6 ± 0.2 22 ± 10 >100

n.d.: value not determined