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. Author manuscript; available in PMC: 2016 Apr 8.
Published in final edited form as: J Med Chem. 2015 Aug 10;58(16):6481–6493. doi: 10.1021/acs.jmedchem.5b00494

Table 1.

Inhibitory Activity and Selectivity of Flavone Derivatives toward P450 1A2a

Compound Short
Name
Structure Ki (μM) Selective Index
(SI)
1A1 1A2 1B1 1A1/1A2 1B1/1A2
Furafylline graphic file with name nihms-770948-t0012.jpg >200 68.0
±13.2
>200 >2.9 >2.9
α-Naphtho
flavone
αNF graphic file with name nihms-770948-t0013.jpg 0.045
±0.010
0.020
±0.005
0.016
±0.002
2.3 0.8
2 78PF graphic file with name nihms-770948-t0014.jpg 0.27
±0.02
0.058
±0.018
0.053
±0.032
4.7 0.9
3 78FF graphic file with name nihms-770948-t0015.jpg 0.43
±0.19
0.030
±0.002
0.18
±0.05
14 6.0
5 5H78PF graphic file with name nihms-770948-t0016.jpg 0.11
±0.02
0.014
±0.004
0.0056
±0.0020
7.9 0.4
8 5H78FF graphic file with name nihms-770948-t0017.jpg 0.47
±0.12
0.044
±0.023
0.10
±0.06
11 2.3
11 78PyF graphic file with name nihms-770948-t0018.jpg 0.040
±0.008
0.076
±0.011
0.12
±0.02
0.5 1.8
12 78DOF graphic file with name nihms-770948-t0019.jpg 1.23
±0.22
0.090
±0.034
0.48
±0.21
14 5.3
a

The Ki values are represented as the mean ± SD μM of three independent experiments.