Table 1: Half-lives (t1/2) of triazene
prodrugs (17a-17g)
in PBS buffer, 80% human plasma and in the presence of tyrosinase
(100 U/mL) at 37ºC.
Compound
|
R |
R’ |
t1/2 |
||
7.4 buffer* (h) |
80% human plasma* (h) |
Tyrosinase** (min) |
|||
17a |
CH3CO |
H |
a |
b |
13.0 |
17b |
CO2Et |
H |
a |
71.5 |
12.9 |
17c |
CN |
H |
a |
b |
11.8 |
17d |
Me |
H |
364 |
b |
18.2 |
17e |
CH3CO |
OH |
15.1 |
9.30 |
9.9 |
17f |
CO2Et |
OH |
20.8 |
14.7 |
6.1 |
17g |
Me |
OH |
b |
5.66 |
8.4 |
*substrate concentration 10-5 M; **
substrate concentration 5 x 10-5 M.
aStable for
15 days; bStable for 2 days.