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. Author manuscript; available in PMC: 2014 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2012 Dec 11;21(3):618–631. doi: 10.1016/j.bmc.2012.11.050

Table 2.

Effect of substituent at R3

graphic file with name nihms428062u5.jpg
Entry R3 IC50 (μM)a
A549 Lung H460 Lung MCF-7 Breast MDA-MB-231 Breast OVCAR-3 Ovarian PC-3 Prostate
15a Ph NE NE NE NE NE NE
15b 4-MeO-Ph NE NE NE NE NE NE
15c 4-MeO- C6H4CH2CH2 NE NE NE NE NE NE
15d CH2CH3 NE NE NE NE NE NE
15e CH2COOEt 33.50 34.50 NE 37.00 NE NE
15f CH2CH2Cl 8.63 7.90 NE NE NE 9.33
15g PhCH2 1.7 1.8 7.0 2.3 5.0 4.05
15h 4-F- C6H4CH2 1.65 1.5 4.05 2.5 9.0 2.1
15i 4-Cl- C6H4CH2 0.78 0.85 2.38 0.97 0.88 0.92
15j 4-Br- C6H4CH2 0.63 0.57 1.02 1.16 1.62 0.98
15k 3-MeO- C6H4CH2 1.50 1.55 6.00 2.60 2.50 5.15
15l 2-MeO- C6H4CH2 NE NE NE NE NE NE
15m 3-F- C6H4CH2 1.20 1.24 1.64 2.70 3.18 1.83
15n 3,4-Di-F- C6H3CH2 0.99 0.74 1.75 1.70 2.27 1.59
15o 3-Cl- C6H4CH2 0.89 1.00 2.49 1.15 1.07 0.97
15p 3-Br- C6H4CH2 1.37 1.17 1.85 1.53 1.54 2.57
15q 3-F3C- C6H4CH2 3.19 3.10 4.31 4.61 3.68 8.30
15r 4-OH- C6H4CH2 4.21 4.68 6.58 3.15 4.36 5.12
15s 4-(CH3OCH2CH2)O-C6H4CH2 4.89 5.14 14.77 5.61 5.45 6.70
15t 4-(HOCH2CH2)O- C6H4CH2 12.34 10.94 27.16 10.58 13.15 19.69
15u 3-Pyridylmethyl 8.05 8.30 19.83 8.68 9.89 26.87
15v 4-(CH3)2N- C6H4CH2 8.81 8.44 15.10 8.82 9.43 202.18
15w CH2CH2Piperidinyl NE NE NE NE NE NE
15x CH2CH2Morpholinyl NE NE NE NE NE NE
a

NE - Not effective. Maximum dose did not inhibit the growth/proliferation by ≤ 75%