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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 5.

Anti-proliferative activity of non-sugar analogues.

graphic file with name nihms295690t5.jpg
Compound
(IC50, µM)
X Y R SKBr3 MCF-7 LNCAP-LN3 PC3-MM2
6a41 H CH3 H 8.88 ± 0.48a 6.93 ± 0.48a 3.21 ± 1.78b 5.36 ± 2.71b
12a41 H CH3 COCH3 0.98 ± 0.02 1.40 1.50 ± 1.00 2.85 ± 1.66
8532 H CH3 Noviose 7.50 ± 0.80 18.70 ± 1.44 NT NT
73a41 H CH3 Ms 7.33 ± 0.96 8.85 ± 0.88 19.96 ± 42.67 >100
74a41 H CH3 Ts > 100 > 100 0.58 ± 1.34 >100
69a H CH3 CONH2 3.02 ± 0.56 1.16 ± 0.08 2.61 ± 1.09 6.37 ± 4.31
70a41 H CH3 CONHMe 2.40 ± 0.16 1.72 ± 0.16 3.75 ± 0.76 5.22 ± 2.16
71a H CH3 CONMe2 39.85 ± 0.48 74.35 ± 3.92 5.40 ± 6.58 >100
72a H CH3 PO(OMe)2 > 100 > 100 3.65 ± 5.73 >100
6b OCH3 CH3 H 3.23 ± 1.20 11.70 ± 1.92 15.79 ± 32.60 11.23 ± 30.70
12b OCH3 CH3 COCH3 5.72 ± 0.02 1.50 ± 0.24 1.05 ± 0.59 1.69 ± 2.05
8633 OCH3 CH3 Noviose 58.80 ± 1.04 > 100 26.57 ± 67.44 >100
73b OCH3 CH3 Ms > 100 > 100 >100 NT
74b OCH3 CH3 Ts > 100 > 100 NT >100
69b OCH3 CH3 CONH2 6.83 ± 0.24 6.29 ± 0.88 3.55 ± 3.44 2.62 ± 2.04
70b OCH3 CH3 CONHMe 1.53 ± 0.16 7.78 ± 1.68 4.77 ± 8.37 3.13 ± 2.34
71b OCH3 CH3 CONMe2 6.17 ± 1.68 34.4 ± 7.20 12.75 ± 0.32d 4.04 ± 16.68
72b OCH3 CH3 PO(OMe)2 26.48 ± 0.80 24.22 ± 2.40 1.36 ± 2.80 31.32 ± 54.87
6c H OCH3 H > 100 5.32 ± 0.08 6.18 ± 7.43 >100
12c H OCH3 COCH3 20.50 ± 1.28 8.62 ± 2.00 14.62 ± 23.63 19.33 ± 50.90
8733 H OCH3 Noviose 13.90 ± 0.96 9.00 ± 4.32 0.11 ± 0.02 1.44 ± 0.32
73c H OCH3 Ms >100 >100 0.87 ± 1.32 NT
74c H OCH3 Ts >100 >100 0.11 ± 4.68 NT
69c H OCH3 CONH2 76.83 ± 1.84 5.56 ± 0.24 4.83 ± 3.87 >100
70c H OCH3 CONHMe >100 6.54 ± 1.84 2.37 ± 1.44 1.68 ± 1.89
71c H OCH3 CONMe2 >100 >100 15.73 ± 14.09 11.57 ± 10.04
72c H OCH3 PO(OMe)2 18.07 ± 2.88 >100 6.58 ± 4.14 11.46 ± 6.54
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.