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. Author manuscript; available in PMC: 2012 Jun 9.
Published in final edited form as: J Med Chem. 2011 May 9;54(11):3839–3853. doi: 10.1021/jm200148p

Table 3.

Anti-proliferative activity of azasugar analogues.

graphic file with name nihms295690t3.jpg
Compound
(IC50, µM)		 R X Y R’ SKBr3 MCF-7 LNCAP-LN3 PC3-MM2
48a A H CH3 H 1.61 ± 0.05a 1.73a 4.27 ± 0.05b,d 4.40 ± 0.06b,d
48b A H OCH3 H 3.07 ± 0.78 1.43 ± 0.37 6.45 ± 2.70d 4.88 ± 2.20
48c A OCH3 CH3 H 1.21 ± 0.07 1.68 ± 0.04 5.40 ± 9.99 3.57 ± 0.71d
50a A H CH3 Ac >50 >50 0.90 ± 0.59 3.73 ± 0.67
51a A H CH3 CH3 2.92 ± 1.33 5.29 ± 0.23 1.22d 1.73 ± 1.80
51b A H OCH3 CH3 3.42 ± 0.45 1.65 ± 0.28 0.36 ± 0.14 0.98 ± 0.40
51c A OCH3 CH3 CH3 1.96 ± 0.48 5.27 ± 0.22 4.49 ± 0.17d 3.87 ± 0.03d
52a B H CH3 H 2.91 ± 0.90 2.07 ± 0.86 4.90 ± 9.16 6.33 ± 4.12
52b B H OCH3 H 8.98 ± 0.44 10.17 ± 0.02 12.19 ± 6.30 14.43 ± 7.39
52c B OCH3 CH3 H 3.65 ± 0.22 3.34 9.45 ± 5.90 6.84 ± 2.80
53a C H CH3 Ac >50 >50 1.23 ± 0.67 3.42 ± 1.24
54a B H CH3 Ac 10.79 ± 0.08 9.18 ± 0.60 0.71 ± 0.54 2.22 ± 1.04
55a B H CH3 CH3 3.92 ± 0.32 1.85 ± 0.02 0.59 ± 0.54 2.99 ± 1.27
55b B H OCH3 CH3 6.64 ± 0.54 11.02 ± 1.12 1.50 ± 0.62 3.52 ± 1.43
55c B OCH3 CH3 CH3 2.77 ± 0.90 2.01 ± 0.46 4.69 ± 0.57d 4.17 ± 0.16d
57a C H CH3 H 1.16 ± 0.16 1.63 ± 0.28 3.02 ± 0.97d 2.57 ± 1.13
57b C H OCH3 H 2.61 ± 0.37 3.29 ± 0.42 12.72 ± 3.25 10.43 ± 2.15
57c C OCH3 CH3 H 2.27 ± 0.61 2.90 ± 0.67 3.66d 2.59 ± 13.91
59a D H CH3 H 1.19 ± 0.06 1.47 ± 0.02 3.38 ± 1.25 4.12 ± 1.29
59b D H OCH3 H 1.79 3.23 ± 0.20 10.85 ± 5.92 8.47 ± 4.28
59c D OCH3 CH3 H 1.20 ± 0.08 2.82 ± 1.10 5.27 ± 22.18 4.02 ± 2.13
60a C H CH3 CH3 2.06 ± 0.57 5.04 ± 0.02 1.22 ± 0.17d 4.23 ± 1.68
60b C H OCH3 CH3 1.40 ± 0.14 1.38 ± 0.14 1.78 ± 0.80 2.16 ± 1.28
60c C OCH3 CH3 CH3 1.49 ± 0.06 1.41 ± 0.13 10.48 ± 5.46d 6.86 ± 2.92d
61a41 D H CH3 CH3 1.34 ± 0.18 1.51 ± 0.24 4.12 ± 0.16d 3.13 ± 0.67
61b D H OCH3 CH3 0.97 ± 0.07 1.39 ± 0.28 4.75 ± 2.03 3.71 ± 1.27
61c D OCH3 CH3 CH3 1.19 ± 0.17 1.79 ± 0.09 4.17 ± 0.15d 2.84 ± 1.88
a

Values represent mean ± standard deviation for at least two separate experiments performed in triplicate.

b

Values represent mean ± standard deviation from dose response curves for at least two separate experiments performed in duplicate.