. 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 4.

EGFR^L858R/T790M enzyme and cell potency of azaquinazolinones 31-32 and F-quinazolinones 33-35


Cpd	X	Y	Z	Enzyme IC₅₀ (nM)	L858R/T790M Cell IC₅₀ (μM)	L858R/T790M Cetux co-dosing Cell IC₅₀ (μM)	L858R/T790M /C797S Cell IC₅₀ (μM)
7				0.9	1.00	0.020	0.18
31	N	CH	CH	0.6	1.71	0.016	0.09
32	CH	N	CH	1.9	1.14	0.023	0.31
33	CH	CF	CH	0.6	0.81	0.010	0.15
34	CF	CH	CH	0.1	0.32	0.003	0.02
35	CH	CH	CF	1.4	3.00	0.073	0.28