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. Author manuscript; available in PMC: 2014 Feb 1.
Published in final edited form as: Eur J Med Chem. 2012 Dec 5;60:456–468. doi: 10.1016/j.ejmech.2012.11.041

Table 2.

Enzymatic properties of selected N3-substituted dThd analogues.

Compounds Km (^M) ± SD1 kcat (S-1) ± SD1 rkcat/Km (%)
dThd 4.9 ± 1.2 0.46 ± 0.03 100.0
N5-2OH 41.5 ± 10.0 0.42 ± 0.03 10.8
9a 37.3 ± 7.0 0.45 ± 0.03 12.9
9b1/2 31.8 ± 8.4 0.44 ± 0.03 14.9
9c1/2 55.2 ± 15.8 0.39 ± 0.04 7.6
9d1/2 56.3 ± 13.2 0.47 ± 0.04 8.9
11a 14.0 ± 2.4 0.34 ± 0.02 26.0
11b1/2 35.6 ± 10.8 0.35 ± 0.03 S 10.7
11c1/2 79.9 ± 36.4 0.37 ± 0.06 5.0
11d1/2 17.4 ± 5.4 0.32 ± 0.02 19.7
1

Data represent the means of three replicates ± SD