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. 2018 Apr 20;8(27):15009–15020. doi: 10.1039/c8ra00465j

Inhibitory potency of 3-hydroxy-2-arylbenzo[h]quinolin-4(1H)-ones 3a–d, 2-arylbenzo[h]quinolin-4(1H)-one 3eand its chemical isomers 4a,b against CYP1B1, CYP1A1, and CYP1A2.

graphic file with name c8ra00465j-u2.jpg
Compound R1 R IC50 values (nM) IC50 ratio
1B1 1A1 1A2 1A1/1B1 1A2/1B1
3a OH H 86.7 897.7 >5000 10.4 >57.7
3b OH o-F 85.9 1783 >5000 20.8 >58.2
3c OH p-OH 141.7 525.1 >5000 3.7 >35.3
3d OH p-F 93.3 333.5 >5000 3.6 >53.6
3e H H 17.3 103.2 483.5 6.0 27.9
4a OH 7.6 18.5 146.9 2.4 19.3
4b OCH3 NIa NI NI
a

NI = no inhibition.