Table 3. Kinase Inhibitory Assay of the Newly Synthesized Derivatives 5–7 in Comparison with Erlotinib and AZD9291 against EGFRWT and Mutant EGFRT790Ma.
IC50 (mean ± SEM) (μM) |
||
---|---|---|
compound no. | EGFRWT | EGFRT790M |
erlotinib | 0.09 ± 0.05 | 0.55 ± 0.10 |
AZD9291 | 0.52 ± 0.03 | 0.03 ± 0.01 |
5a | 0.25 ± 0.01 | 0.17 ± 0.05 |
5b | 0.22 ± 0.15 | 0.13 ± 0.11 |
5c | 0.24 ± 0.30 | 0.14 ± 0.50 |
6a | 0.18 ± 0.10 | 0.12 ± 0.18 |
6b | 0.08 ± 0.05 | 0.09 ± 0.01 |
6c | 0.15 ± 0.02 | 0.13 ± 0.07 |
7 | 0.22 ± 0.05 | 0.18 ± 0.11 |
IC50: compound concentration required to inhibit the enzymes’ activities by 50%; SEM: standard error mean; each value is the mean of three independent values.