Table 3.
Tri- and tetra-substituted coumarins and their CAR activation.
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Compound | R1 | R2 | R3 | R4 | CAR Activation Fold a | Ref |
54 | -OCH3 | -OCH3 | -OCH3 | H | −19% ± 3% | [39,44] |
55
fraxinol |
-OCH3 | -OH | -OCH3 | H | −17% ± 2% | [39] |
56 | -OCH3 | H | -OCH3 | -OCH3 | −14% ± 2% | [39] |
57
leptodactylone |
-OCH3 | H | -OCH3 | -OH | 2% ± 4% | [39] |
58 | H | -OCH3 | -OCH3 | -OCH3 | 0% ± 2% | [52] |
59 | H | -OCH3 | -OCH2O- | 36% ± 23% | [17,53] | |
60 | -OCH3 | -OCH3 | -OCH2O- | 12% ± 1% | [17,53] |
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%.