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. Author manuscript; available in PMC: 2019 Jan 29.
Published in final edited form as: Biochem Biophys Res Commun. 2018 Jan 5;496(1):205–211. doi: 10.1016/j.bbrc.2018.01.027

Table 2.

MEKK2 inhibitory activity for Compound 1 derivatives

graphic file with name nihms934001u1.jpg
Compound R′1 R′2 R′3 R′4 R′5 R IC50 (nM)a
1a H H OMe H H OMe >10,000
1b H Cl OH H H OMe 60b
1c H Me OH H H OMe 362
1d H OH OH H H OMe 361
1e H F OH H H OMe 115
1f CF3 H OH H H OMe 38
1g Me H OH H H OMe 28
1h F H OH H H OMe 39
1i F F OH H H OMe 36
1j H F OH F H OMe 27
1k F H OH H F OMe 8
1l H H OH H H OEt 130b
1m H H OH H H OPropyl 371c
1n H H OH H H OIsopropyl 502b
1o H H OH H H F 2102
1p H H OH H H Br 152b
1q H H OH H H OH 766
1r CF3 H OH H H OEt 18c
1s Me H OH H H OEt 16
a

IC50 values are the mean of two to five independent determinations using the intrinsic ATPase MEKK2 activity assay.

b

Apparent solubility problems observed at compound concentrations >1 μM.

c

Apparent solubility problems observed at compound concentrations >0.3 μM.