Table 4. In Vitro Enzyme Inhibitory Activity of the Synthesized Compound on the Triple Mutant EGFR and the Number of Structural Descriptors Contained in the Compounda.
| compound | EGFRL858R/T790M/C797S IC50 (μM) | EGFRDel19/T790M/C797SIC50 (μM) | fr_aniline | NumAromaticHeterocycles |
|---|---|---|---|---|
| 4a | 1.221 ± 0.031 | 1.432 ± 0.022 | 1 | 1 |
| 4b | 0.736 ± 0.044 | 0.220 ± 0.002 | 1 | 1 |
| 4c | 0.277 ± 0.028 | 0.089 ± 0.004 | 1 | 1 |
| Angew-2017 | Ndb | 0.018 | 1 | 2 |
The data are the mean ± SD of at least three independent experiments.
Nd: no data.