Table 4. Structures and PI3K Enzyme and Cell Inhibitory Potencies of Compounds 27–37.

compd	R1	PI3Kα IC50 (nM)	selectivity folds over PI3Kβ/δ/γ	cellulara IC50 (nM)
27	–OCH2CH3	13.7	153/–/–	116
28	–OCH(CH3)2	–	–/–/–	387
29	– OCH(CH2)2	–	–/–/–	55.3
30 (rac)	–OCF3	22.8	94.9/–/–	>1000
31 (rac)	–CF3	0.6	196/–/–	972
32	–CH3	3.0	406/17/21	397
33	–CH2CH3	6.0	309/13.8/14.4	347
34	–CH2OH	30.0	>334/17.9/12.5	>1000
35	–CH2OCH3	>1000	–/–/–	>1000
36	–NH2	19.3	283/–/–	>1000
37	–N(CH3)2	8.4	59.5/–/–	–

^aMCF-7 pAkt^S473 inhibitory IC₅₀ values.