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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 3.

Activity and cytotoxicity of T3SS inhibitors with alternative linkers.

graphic file with name nihms660087t3.jpg
Compound
#
X R secretion
IC50 (µM)
translocation
IC50 (µM)
translocation
CC50 (µM)
1 O 3,4-methylenedioxy 7.8 ± 2.0 11 ± 2 >100
2 O 4-F 9.8 ± 2.9 6.7 ± 1.0 59 ± 16
20a S 3,4-methylenedioxy 7.8 ± 2.0 >100 >100
20b S 4-F 7.8 ± 2.0 >100 >100
21a SO2 3,4-methylenedioxy >100 n.d. n.d.
21b SO2 4-F >100 n.d. n.d.
23a NH 3,4-methylenedioxy 45 ± 4 >100 >100
23b NH 4-F 34 ± 8 32 ± 5 >100
25a CH2 3,4-methylenedioxy >100 n.d. n.d.
25b CH2 4-F >100 n.d. n.d.

n.d.: value not determined