Table 1.
Prodrug |
R1 |
R2 |
PB pH=7.3 t 1/2 [h] |
CEM/0 cell extracts t 1/2 [h] |
---|---|---|---|---|
3 ae |
C2H5 |
n‐C14H29 |
59 |
0.8 |
3 be |
n‐C4H9 |
n‐C14H29 |
45 |
2.5 |
3 de |
n‐C6H13 |
n‐C14H29 |
61 |
2.3 |
3 ce |
iso‐C4H9 |
n‐C14H29 |
64 |
3.8 |
3 bf |
n‐C4H9 |
n‐C15H31 |
49 |
3.1 |
3 bg |
n‐C4H9 |
n‐C17H35 |
50 |
3.3 |
3 bh |
n‐C4H9 |
MEEES |
22 |
0.8 |
3 eh |
n‐C14H29 |
MEEES |
65 |
1.1 |
3 ei |
n‐C14H29 |
MEEEG |
86 |
2.4 |
D4T |
/ |
/ |
>40 |
n.a.[a] |
D4TTP31 |
/ |
/ |
>40 |
0.6 |