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. 2022 Apr 15;13(5):827–832. doi: 10.1021/acsmedchemlett.2c00064

Table 3. SAR of Biaryl Side Chain Derivatives with Second Phenyl Ring Meta to the Amide.

graphic file with name ml2c00064_0010.jpg

entry R1 R2 R3 R4 R5 IC50
7h H OMe H H H 4.83 ± 0.9 μM
16a H H H H H >10 μM
16b OMe H H H H 9.65 ± 0.1 μM
16c OH H H H H >10 μM
16d OMe OMe H H H >10 μM
16e OMe H H H OMe 9.05 ± 0.4 μM
16f H OH H H H >10 μM
16g H N(Me)2 H H H 3.36 ± 0.3 μM
16h H NH2 H H H 7.23 ± 0.6 μM
16i H CH2OH H H H >10 μM
16j H Cl H H H >10 μM
16k H F H H H >10 μM
16l H CF3 H H H >10 μM
16m H CF3 Cl H H >10 μM
16n H Cl Cl H H >10 μM
16o H H Cl H H >10 μM
16p H H CF3 H H >10 μM
16q H H OMe H H >10 μM
16r H H OH H H 6.39 ± 1.4 μM