Skip to main content
. Author manuscript; available in PMC: 2020 Sep 15.
Published in final edited form as: Bioorg Med Chem Lett. 2019 Jul 10;29(18):2695–2699. doi: 10.1016/j.bmcl.2019.07.012

Table 2.

Results of alcohol replacement of lapatinib and gefitinib (1-12).

graphic file with name nihms-1537187-t0005.jpg
Compound X R1 R2 R3 Mtb signala (μM) WS-1b
1.25 2.5 5 10 20 (μM)
1 N OH H H 0.95 0.94 0.96 0.90 0.80 26
2 N H OH H 0.90 0.90 0.89 0.88 0.89 >100
3 N OH OH H 0.95 0.93 0.91 0.76 0.69 8.8
4 N OMe H H 1.04 1.07 0.89 0.83 0.62 >100
5 N H OMe H 1.05 1.12 0.99 0.87 0.64 >100
6 N OMe OMe H 1.04 1.04 0.83 0.77 0.6 >100
7 CH OH H H 0.95 0.86 0.66 0.42 0.37 2.5
8 N OH H 4-F 0.86 0.76 0.64 0.44 0.32 >100
9 N OH H 3-F 0.76 0.64 0.49 0.39 0.25 12
10 N OH H 2-F 0.89 0.82 0.63 0.46 0.28 28
11 N H OH 4-F 0.94 1.01 0.90 0.89 0.83 >100
12 N OH OH 4-F 1.04 1.14 1.00 0.89 0.76 >100
a

Relative luminescence measured at 3 days after treatment. Values = RLU(sample)/RLU(no compound) at μM concentrations and no effect at 0.625 μM;

b

IC50 (mean average n=4), 48 h