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. Author manuscript; available in PMC: 2018 Sep 23.
Published in final edited form as: ChemMedChem. 2016 Oct 5;11(21):2410–2421. doi: 10.1002/cmdc.201600417

Table 1.

Stability and NTR activation of compounds 1a, 1b, and 2a–2c.

Compd Stability [%][a] NTR activation[b]
t12 [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%
[a]

Aqueous stability of compound solutions (2.5 μm) after 24 h in phosphate buffer (10 mm, pH 7.4, 37°C), determined by HPLC.

[b]

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.