Table 2. N5-Alkyl Group Exploration.

^aSee ref (17).

^bCellular IC₅₀ run in PC-3 cell line measuring p-AKT S473.

^cSelectivity is the ratio of the PI3Kα enzyme IC₅₀ over the mTOR enzyme IC₅₀ as described in ref (10).

^dHLM apparent intrinsic clearance scaled to units of mL min^–1 kg^–1.

^e2:1 mixture of THF diastereomers.