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. Author manuscript; available in PMC: 2016 Apr 8.
Published in final edited form as: J Med Chem. 2015 May 22;58(11):4713–4726. doi: 10.1021/acs.jmedchem.5b00470

Table 3.

Antiproliferative Activity and Cytotoxicity of Selected 1,5-Diheteroarylpenta-1,4-dien-3-ones

compd IC50 (μM)a
PC-3b
DU145,c WST-1 LNCaP,d WST-1 HeLae
WST-1 TB WST-1 TB
curcumin   25.43 ± 2.15   12.36 ± 0.04 26.23 ± 0.65   13.61 ± 2.69   12.11 ± 0.67   10.46 ± 1.97
6 1.07 ± 0.38 0.91 ± 0.08 0.59 ± 0.10 0.52 ± 0.25
7 1.53 ± 0.05 0.66 ± 0.14 0.78 ± 0.12 0.40 ± 0.05
8 0.68 ± 0.08 0.37 ± 0.02 0.49 ± 0.03 0.23 ± 0.04
9 0.71 ± 0.06 0.55 ± 0.14 0.59 ± 0.03 0.35 ± 0.04
10 0.90 ± 0.07 0.85 ± 0.14 1.13 ± 0.07 0.65 ± 0.02 0.59 ± 0.13
12 0.31 ± 0.06 0.29 ± 0.05 0.24 ± 0.05 0.19 ± 0.08 0.15 ± 0.13
13 0.69 ± 0.07 0.62 ± 0.13 0.58 ± 0.17 0.36 ± 0.02 0.25 ± 0.05
14 0.71 ± 0.06 0.71 ± 0.11 0.57 ± 0.17 0.41 ± 0.02 0.23 ± 0.04
15 0.60 ± 0.05 0.53 ± 0.12 0.39 ± 0.11 0.33 ± 0.03
19 0.51 ± 0.06 0.45 ± 0.13 0.31 ± 0.14 0.14 ± 0.10 0.21 ± 0.03
22 0.84 ± 0.11 0.96 ± 0.02 0.46 ± 0.25 0.67 ± 0.05
24 0.71 ± 0.04 1.14 ± 0.00 0.60 ± 0.05 0.47 ± 0.26 0.92 ± 0.17
26 0.47 ± 0.08 0.47 ± 0.16 0.23 ± 0.17 0.20 ± 0.01 0.25 ± 0.05
30 0.73 ± 0.20 1.51 ± 0.28 0.67 ± 0.31 0.71 ± 0.15
32 0.47 ± 0.13 0.41 ± 0.04 0.66 ± 0.20 0.41 ± 0.13 0.42 ± 0.20 0.48 ± 0.15
36 0.21 ± 0.03 0.39 ± 0.13 0.34 ± 0.08 0.27 ± 0.06 0.14 ± 0.04 0.43 ± 0.20
37 0.52 ± 0.01 0.42 ± 0.13 0.38 ± 0.08 0.23 ± 0.01
38 0.34 ± 0.04 0.45 ± 0.22 0.52 ± 0.12 0.17 ± 0.01
39 0.40 ± 0.04 0.51 ± 0.14 0.58 ± 0.15 0.20 ± 0.04
40 0.37 ± 0.04 0.70 ± 0.22 0.86 ± 0.20 0.32 ± 0.04
41 0.64 ± 0.22 1.83 ± 0.33 1.16 ± 0.23 0.59 ± 0.10
43 0.23 ± 0.02 0.14 ± 0.01 0.53 ± 0.10 0.45 ± 0.02 0.16 ± 0.02 0.14 ± 0.05
44 0.22 ± 0.01 0.21 ± 0.07 0.43 ± 0.03 0.38 ± 0.07 0.14 ± 0.02 0.15 ± 0.02
45 0.34 ± 0.10 0.24 ± 0.06 0.83 ± 0.14 0.79 ± 0.10 0.23 ± 0.02 0.23 ± 0.07
46 0.30 ± 0.06 0.70 ± 0.24 0.89 ± 0.04 0.70 ± 0.08 0.27 ± 0.03 0.69 ± 0.13
47 0.26 ± 0.03 0.93 ± 0.22 0.83 ± 0.15 0.54 ± 0.12 0.18 ± 0.02 0.93 ± 0.29
48 0.79 ± 0.20 >2 0.92 ± 0.07 0.54 ± 0.12 0.84 ± 0.26
a

IC50 is the drug concentration effective in inhibiting 50% of the cell viability measured by WST-1 cell proliferation assay (WST-1) or trypan blue exclusion assay (TB) after 3 days exposure.

b

Human androgen-insensitive prostate cancer cell line.

c

Human androgen-insensitive prostate cancer cell line.

d

Human androgen-sensitive prostate cancer cell line.

e

Human aggressive cervical cancer cell line.