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. Author manuscript; available in PMC: 2019 May 1.
Published in final edited form as: Bioorg Med Chem Lett. 2018 Mar 13;28(8):1278–1282. doi: 10.1016/j.bmcl.2018.03.033

Table 1.

In vitro cytotoxicity of β-carboline chalcones 12a–g and their bromides 13a–i against a panel of cancer cells and a non-cancerous cell line (IC50 in μM).

graphic file with name nihms-1010042-t0001.jpg
Compd Ar R BxPC-3 HeLa C4–2 PC-3 HEK293T MDA-MB-231 NIH3T3
12a C6H5 72.02 ± 2.75 82.36 ± 3.43 80.25 ± 5.46 93.02 ± 3.54 65.58 ± 2.84 71.11 ± 4.12 >100
12b 4-CH3C6H4 >100 >100 >100 >100 >100 >100 >100
12c 4-CH3OC6H4 >100 >100 >100 >100 >100 >100 >100
12d 3,4-(CH3O)2C6H3 >100 >100 >100 >100 >100 >100 >100
12e 3,4,5-(CH3O)3C6H2 70.78 ± 4.98 75.2 ± 3.6 71.6 ± 4.87 >100 82.1 ± 5.09 71.54 ± 4.3 >100
12f 4-CF3C6H4 ND ND ND ND ND ND ND
12 g 4-(CH3)2NC6H4 ND ND ND ND ND ND ND
13a 4-CH3OC6H4 Benzyl 50.25 ± 4.91 60.14 ± 4.65 65.5 ± 5.58 88.3 ± 7.1 41.4 ± 3.6 52.2 ± 4.95 85.3 ± 5.1
13b 4-CH3OC6H4 n-Butyl 50.79 ± 4.91 44.99 ± 4.32 38.79 ± 4.91 64.99 ± 5.5 35.18 ± 4.1 40.9 ± 3.96 74.6 ± 2.50
13c 4-CH3OC6H4 Propargyl >100 >100 >100 >100 >100 >100 >100
13d 3,4-(CH3O)2C6H3 Benzyl 55.3 ± 3.48 45.25 ± 4.41 42.05 ± 4.35 78.95 ± 6.4 55.14 ± 5.8 48.23 ± 4.69 82.25 ± 3.33
13e 3,4-(CH3O)2C6H3 n-Butyl >100 >100 >100 >100 >100 >100 >100
13f 3,4-(CH3O}2C6H3 Propargyl 30.14 ± 3.41 25.32 ± 2.79 24.4 ± 2.64 29.6 ± 3.1 19.14 ± 2.78 21.2 ± 3.1 72.1 ± 4.12
13 g 3,4,5-(CH3O)3C6H2 Benzyl 20 ± 2.1 22.1 ± 3.23 16.13 ± 4.2 22.02 ± 3.25 17.18 ± 2.98 15.95 ± 3.41 55.23 ± 5.8
13 h 3,4,5-(CH3O)3C6H2 n-Butyl 25.1 ± 3.65 35.56 ± 2.2 39.65 ± 2.98 40.13 ± 3.5 34.4 ± 3.89 32.05 ± 4.0 68.6 ± 6.54
13i 3,4,5-(CH3O)3C6H2 Propargyl 72.02 ± 5.3 70.1 ± 4.9 65.5 ± 5.74 60.98 ± 6.1 55.07 ± 4.4 59.61 ± 4.81 88 ± 3.85
Doxorubicin 13.56 ± 2.21 5.23 ± 1.92 3.2 ± 1.1 10.2 ± 0.98 3.59 ± 1.1 7.85 ± 1.59 21.32 ± 2.56
*

The activity data represent mean values ± SD of experiments conducted in triplicates at three independent times