Table 1.
Compd | Stability [%][a] | NTR activation[b] | ||
---|---|---|---|---|
[min] | Amount of substrate after 15 min [%] |
Product and amount after 25 min |
||
1a | 14 | <1 | 0 | sunitinib, 93% |
1b | 4 | <6 | 10 | sunitinib, 58% |
2a | 88 | <6 | 10 | erlotinib, 44% |
2b | 90 | – | 100 | – |
2c | 76 | <6 | 0 | 2b, 90% |
Aqueous stability of compound solutions (2.5 μm) after 24 h in phosphate buffer (10 mm, pH 7.4, 37°C), determined by HPLC.
Reduction and subsequent fragmentation of compounds (2.5 μm) in phosphate-buffered solutions by incubation with NADH (50 μm) and NTR (1.33 μg mL-1) at 37°C, calculated from the HPLC chromatogram peak areas as a function of time.