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. Author manuscript; available in PMC: 2023 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2022 Apr 1;68:128718. doi: 10.1016/j.bmcl.2022.128718

Table 2.

EGFRL858R/T790M enzyme and Ba/F3 cell activity of isoindolinones (A) and dihydroisoquinolinones (B)

graphic file with name nihms-1852250-t0008.jpg
Cpd Core R1 R2 Enzyme
IC50 (nM)		 L858R/T790M
Cell IC50 (μM)		 L858R/T790M
Cetux co-dosing
Cell IC50 (μM)		 L858R/T790M
/C797S
Cell IC50 (μM)
6 A H N-Me piperazine 0.9 2.56 0.043 -
7 A H N-Me piperidine 0.9 1.00 0.020 0.179
8 A F N-Me piperazine 1.8 1.99 0.044 -
5 A F N-Me piperidine 0.2 1.07 0.020 0.152
9 B F 6, N-Me piperazine 1.1 3.66 0.801 -
10 B F 6, N-Me piperidine 2.2 1.99 0.246 -
11 B F 7, N-Me piperazine 6.8 1.60 0.126 -
12 B F 7, N-Me piperidine 3.2 1.47 0.099 -