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

Inhibitory potency of 2-aryl-2,3-dihydrobenzo[h]quinolin-4(1H)-ones 1a–d and their 3-hydroxy derivatives 2a,b against CYP1B1, 1A1, and 1A2.

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Compound R1 R IC50 values (nM) IC50 ratio
1B1 1A1 1A2 1A1/1B1 1A2/1B1
1a H H 131.4 404.6 952.8 3.1 7.3
1b H 3,4,5-TriOCH3 20.2 44.6 >5000 2.2 >247.5
1c H o-F 139.3 577.5 1097 4.1 7.9
1d H m-F 98.6 493.2 1045 5.0 10.6
2a OH H 259.6 587.9 1411 2.3 5.4
2b OH 3,4,5-TriOCH3 302.5 1161 >5000 3.8 >16.5
ANF — — 5.6 62.8 14.1 11.2 2.5