. 2010 Oct 13;2(1):34–38. doi: 10.1021/ml1001932

Table 3. Biochemical Inhibition of PI3Kα, Inhibition of AKT^Ser473 Phosphorylation, and Antiproliferative Effect in A2780 Cells by 4-Substituted, 2-Morpholino, 6-(2-Aminopyrimid-5-yl) Pyrimidines.

graphic file with name ml-2010-001932_0005.jpg

no.	R	PI3Kα IC₅₀ (μM)	pAKT^Ser473 A2780 EC₅₀ (μM)	A2780 EC₅₀ (μM)
12	quinolin-3-yl-amino	<0.002	0.04	0.15
15	6-phenoxypyridin-3-yl-amino	<0.002	0.11	1.13
16	6-(1-methylpiperidin-4-yloxy)pyridin-3-yl-amino	<0.002	0.01	0.14
17	6-methoxypyridin-3-yl-amino	<0.002	0.09	0.73
18	2-amino-pyrimid-5-yl	0.006		0.23
19	tetrahydro-2H-pyran-4-yl-amino	0.013	0.22	1.96
20	H	0.014	0.13	4.98

Table 3. Biochemical Inhibition of PI3Kα, Inhibition of AKTSer473 Phosphorylation, and Antiproliferative Effect in A2780 Cells by 4-Substituted, 2-Morpholino, 6-(2-Aminopyrimid-5-yl) Pyrimidines.