Skip to main content
. 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 1.

Anti-proliferative activity of various sugar analogues.

graphic file with name nihms295690t1.jpg
Compound
(IC50, µM)
R R1 R2 R3 Anomer X Y SKBr3 MCF-7 LNCAP-LN3 PC3-MM2
14a A OH OH H β H CH3 6.23 ± 0.52a,c 2.56 ± 0.08a 3.59 ± 3.40b NTb
15a A OH OH H α H CH3 6.71± 0.80 42.56 ± 2.48 1.20 ± 0.83 12.88 ± 9.30
14b A OH OH H β H OCH3 1.46 ± 0.46 17.46 ± 1.22 2.29 ± 1.25 10.72 ± 10.85
15b A OH OH H α H OCH3 11.10 ± 0.43 10.85 ± 0.18 NT NT
14c A OH OH H β OCH3 CH3 7.18 ± 0.20 9.50 ± 0.16 12.76 ± 5.12 24.03 ± 17.14
15c A OH OH H α OCH3 CH3 12.52 ± 0.54 64.51 ± 3.52 14.93 ± 9.24 25.37 ± 7.26
17a A OH H H β H CH3 >100 >100 3.75 ± 0.01d 10.05 ± 0.01d
18a41 A OH H H α H CH3 >100 >100 7.34 ± 11.82 NT
20a A H OH H β H CH3 >100 >100 3.11 ± 2.58 >100
21a41 A H OH H α H CH3 9.28 ± 0.04 11.20 ± 0.49 8.56 ± 9.00 NT
20b A H OH H β H OCH3 8.75 ± 0.49 95.77 ± 3.21 11.50 ± 5.66 NT
20c A H OH H β OCH3 CH3 >100 >100 1.49 ± 0.51 1.24d
21c A H OH H α OCH3 CH3 1.37 ± 0.14 >100 3.27 ± 0.09d 2.35 ± 1.11
23a A OH OH CH2OH β H CH3 9.59 ± 0.42 11.07 ± 0.47 3.23 ± 3.76 4.58 ± 2.78
23b A OH OH CH2OH β H OCH3 11.76 ± 0.06 14.34 ± 0.16 6.78 ± 2.25 17.94 ± 10.33
23c A OH OH CH2OH β OCH3 CH3 9.45 ± 0.19 3.37 ± 0.06 4.66 ± 1.48 5.90 ± 2.58
25a B OH OH H β H CH3 12.46 ± 0.52 37.17 ± 1.68 3.65 ± 2.83 NT
25b B OH OH H β H OCH3 7.57 ± 1.05 11.73 ± 0.78 2.60 ± 1.51 10.64 ± 20.83
25c B OH OH H β OCH3 CH3 9.45 ± 0.19 3.37 ± 0.07 4.72 ± 1.48 9.56 ± 2.58
27a B OH H -- β H CH3 >100 >100 NT NT
28a B OH H -- α H CH3 >100 >100 5.34 ± 4.76 NT
30a B H OH -- β H CH3 35.24 ± 1.76 >100 3.72d 10.05 ± 6.75d
31a B H OH -- α H CH3 >100 >100 4.96 ± 10.58 26.79 ± 58.24
33a C OH OH -- β H CH3 2.38 ± 0.06 >100 >100 NT
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.

c

All error values listed represent 95% confidence intervals throughout the manuscript except where indicated

d

Error values listed as standard deviations