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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 7.

Activity and cytotoxicity of T3SS inhibitors with multiple optimizations.

graphic file with name nihms660087t7.jpg
Compound
#		 L Ar secretion
IC50 (µM)		 translocation
IC50 (µM)		 translocation
CC50 (µM)
1 −NHCH2- 3,4-methylenedioxyphenyl 7.8 ± 2.0 11 ± 2 >100
2 −NHCH2- 4-fluorophenyl 9.8 ± 2.9 6.7 ± 1.0 59 ± 16
37a −NHCH2- benzothiophene-5-yl 0.9 ± 0.1 3.6 ± 0.1 >100
37b −NHCH2- indole-5-yl 0.8 ±-0.1 1.9 ± 0.2 >100
37c −NHCH(CH2OH)- 4-fluorophenyl 6.9 ± 0.2 29.3 ± 3.2 75 ± 21