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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 6.

Anti-proliferative activity of optimized analogues.

graphic file with name nihms295690t6.jpg
Compound
(IC50, µM)		 R X Y R’ R” SKBr3 MCF-7 LNCAP-LN3 PC3-MM2
78a A H CH3 C -- 0.48 ± 0.09a 0.57 ± 0.03a 11.83 ± 0.54b 11.40 ± 5.25b
78b A H OCH3 C -- 2.58 ± 0.28 1.86 ± 0.08 12.64 ± 0.32d 7.93 ± 4.18
78c A OCH3 CH3 C -- 0.11 ± 0.01 0.52 ± 0.04 1.47 ± 0.53 0.87 ± 0.46
79a A H CH3 D Ac 0.58 ± 0.04 1.18 ± 0.16 NT 2.12 ± 3.32
79b A H OCH3 D Ac 1.07 ± 0.14 1.64 ± 0.24 NT 3.98 ± 0.06d
79c A OCH3 CH3 D Ac 0.42 ± 0.01 0.58 ± 0.02 NT 1.41 ± 0.04d
80a A H CH3 D H 0.76 ± 0.14 1.09 ± 0.08 NT 1.37 ± 1.42
80b A H OCH3 D H 0.92 ± 0.01 1.54 ± 0.21 NT 3.53 ± 0.01d
80c A OCH3 CH3 D H 0.42 ± 0.01 0.54 ± 0.02 NT 2.26 ± 1.43
82a B H CH3 C -- 1.13 ± 0.01 5.23 ± 0.22 NT 13.69 ± 0.18d
82b B H OCH3 C -- 1.50 ± 0.13 1.41 ± 0.09 4.71 ± 1.23d 8.95 ± 6.11
82c B OCH3 CH3 C -- 0.57 ± 0.09 0.56 NT 2.58 ± 4.47
83a B H CH3 D Ac 0.46 ± 0.15 1.18 ± 0.02 NT 1.42 ± 0.05d
83b B H OCH3 D Ac 0.78 ± 0.17 2.14 ± 0.22 NT 4.59 ± 4.23
83c B OCH3 CH3 D Ac 0.36 ± 0.03 0.70 ± 0.03 NT 1.46 ± 0.03d
84a B H CH3 D H 0.44 ± 0.02 1.35 ± 0.30 NT 1.81 ± 1.22
84b B H OCH3 D H 0.77 ± 0.08 3.26 ± 0.26 NT 9.24 ± 17.79
84c B OCH3 CH3 D H 0.39 ± 0.06 0.80 ± 0.07 NT 1.38 ± 0.02d
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.