Table 2.

Di-substituted coumarins and their CAR activation.

Compound	R1	R2	CAR Activation Fold a	Ref
35 esculetin	OH	OH	−22% ± 12%	[36,44]
36	methyl	methyl	−17% ± 5%	[24]
37 isoscopoletin	OH	O-methyl	−10% ± 6%	[45]
38 scopoletin	O-methyl	OH	−1% ± 5%	[44]
39 scoparone	O-methyl	O-methyl	-	[15,17]
40 ayapin	-OCH2O-		7% ± 2%	[46]
41	-OCH2CH2O-		−50% ± 9%	[47]
42	O-ethyl	O-ethyl	−26% ± 8%	[37]
43	O-acetyl	O-acetyl	−11% ± 2%	[37]
44	O-allyl	O-allyl	−18% ± 15%	New
45	O-propyl	O-propyl	−37% ± 5%	[37]
46	O-n-butyl	O-n-butyl	−39% ± 13%	New
47	O-pentyl	O-pentyl	−10% ± 18%	New
48	O-isopentyl	O-isopentyl	−61% ± 2%	New
49	O-hexyl	O-hexyl	−5% ± 9%	New
50	O-prenyl	O-prenyl	50% ± 1%	[48,49,50]
51	O-geranyl	O-geranyl	−32% ± 11%	New
52 isoscopolin	O-Glc	O-methyl	35% ± 5%	[17,51]
53 scopolin	O-methyl	O-Glc	17% ± 26%	[17]

^a CAR activation fold was calculated: (the luminescence value of the tested compound- the luminescence value of scoparone)/the luminescence value of scoparone (as positive control) × 100%.