Table 1. EC₅₀ Values against Nrf2 Activation of Synthesized Compounds.

compd.	X	R1	R2	Nrf2 EC50 (μM)a
2a	N	-H	-H	>10
2b	N	-H	2′-Cl	>10
2c	N	2-OMe	2′-Cl	6.350 ± 0.039
2d	N	3-OMe	2′-Cl	>10
2e	N	4-OMe	2′-Cl	>10
3a	O	-H	-H	1.040 ± 0.015
3b	O	4-OMe	-H	1.480 ± 0.047
3c	O	2-OMe	2′-Cl	0.076 ± 0.009
3d	O	3-OMe	2′-Cl	0.165 ± 0.026
3e	O	4-OMe	2′-Cl	0.237 ± 0.015
3f	O	2-OMe	3′-Cl	0.698 ± 0.016
3g	O	3-OMe	3′-Cl	0.943 ± 0.050
3h	O	4-OMe	3′-Cl	0.948 ± 0.028
3i	O	2-OMe	4′-Cl	1.334 ± 0.024
3j	O	3-OMe	4′-Cl	1.778 ± 0.030
3k	O	4-OMe	4′-Cl	1.155 ± 0.036
1b		2-OMe	2′-Cl	0.530 ± 0.025
SFNc				0.580 ± 0.024

^aThe Nrf2 functional assay was accomplished by a PathHunter U2OS Nrf2 nuclear translocation cell line (93-0821C3, DiscoveRx). U2OS cells were plated at 13,000 cells/well in triplicate with various compound concentrations for 6 h. Nrf2 translocation, which is activation-dependent, was determined using a cell-based functional assay of the mean ± standard error half maximal effective concentration (EC₅₀) values.

^bCompound 1 developed as an Nrf2 activator in a previous study.²⁴

^cSFN, sulforaphane: a well-known potent Nrf2 activator.