Table 4.

Activity and cytotoxicity of T3SS inhibitors with varying substituents at the benzylic position.

Compound #	R	R’	secretion IC50 (µM)	translocation IC50 (µM)	translocation CC50 (µM)
2	−H	−H	9.8 ± 2.9	6.7 ± 1.0	59 ± 16
27a	−Me	−H	6.0 ± 1.2	23 ± 1	>100
27b*	−Me (S)	−H	4.2 ± 0.2	>32	32 ± 1
27c*	−Me (R)	−H	2.6 ± 0.9	>97	97 ± 9
27d	−Me	−Me	3.3 ± 0.6	>100	>100
27e	−CH2CH2-		5.4 ± 0.2	>28	28 ± 14
27f	−Et	−H	4.4 ± 0.6	25 ± 1	>100
27g	−nPr	−H	3.9 ± 0.7	>100	>100
27h	−iPr	−H	3.5 ± 1.9	>100	>100
27i	−cPr	−H	3.0 ± 1.8	8.3 ± 2.3	>100
27j	−nBu	−H	4.5 ± 0.4	>100	>100
27k	−cBu	−H	2.7 ± 0.7	>100	>100
27l	−CH2OH	−H	6.0 ± 1.5	>18	18 ± 2
27m	−CN	−H	5.8 ± 1.0	12 ± 2	>100
27n	−COOMe	−H	8.1 ± 2.0	>100	>100
27o	−COOH	−H	>100	n.d.	n.d.

n.d.: value not determined

^*Compounds synthesized using (R)-acid