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Table 1 In vitro cytotoxic activities of the compounds against human cancer cell lines and normal cells

From: Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

Entry Compd
no.
Substituents In vitro cytotoxicity IC a50 (μg/mL)
R1 R2 X Z Ar NCI-H460 A549 NCI-H1975 HL-7702 MDCK
1 4a H H N CH 3-CF3Ph > 40 > 40 > 40 > 40 > 40
2 4b H CH3 N CH 3-CF3Ph 36.68 ± 2.80 > 40 > 40 > 40 > 40
3 4c H CH3CH(OH)CH2 N CH 3-CF3Ph 20.63 ± 1.37 26.31 ± 3.22 27.25 ± 2.76 19.73 ± 0.45 16.98 ± 0.84
4 4d H CH3COCH2 N CH 3-CF3Ph 4.07 ± 1.30 13.09 ± 2.45 12.82 ± 1.59 26.87 ± 0.95 13.45 ± 0.29
5 4e 3-CH3-5-Cl H C N 3-CF3Ph > 40 > 40 > 40 > 40 > 40
6 4f 3-CH3-5-Cl CH3 C N 3-CF3Ph > 40 > 40 > 40 > 40 > 40
7 4g H H N N 3-CF3Ph 9.17 ± 2.02 20.12 ± 0.48 10.85 ± 2.22 9.86 ± 0.34 13.04 ± 1.27
8 4h H CH3 N N 3-CF3Ph 9.31 ± 2.66 17.18 ± 3.40 12.44 ± 2.52 11.62 ± 2.08 11.06 ± 0.24
9 4i H CH3CH(OH)CH2 N N 3-CF3Ph 13.08 ± 4.49 16.53 ± 3.53 9.15 ± 1.64 14.51 ± 2.19 11.62 ± 0.06
10 4j 4,5-(CH=CH–CH=CH)– H CH N 3-CF3Ph 38.44 ± 3.95 24.79 ± 3.00 25.20 ± 3.35 18.09 ± 1.63 14.30 ± 0.66
11 4k 4,5-(CH=CH–CH=CH)– CH3 CH N 3-CF3Ph > 40 35.30 ± 2.19 > 40 > 40 > 40
12 4l 3-CH3-5-Cl H C CH 3-CF3Ph > 40 > 40 > 40 > 40 > 40
13 4m 3-CH3-5-Cl CH3 C CH 3-CF3Ph 6.85 ± 0.23 6.77 ± 0.86 10.83 ± 1.02 21.44 ± 1.79 21.25 ± 3.59
14 4n 4,5-(CH=CH–CH=CH)– H CH CH 3-CF3Ph > 40 > 40 > 40 > 40 14.44 ± 0.01
15 4o 4,5-(CH=CH–CH=CH)– CH3 CH CH 3-CF3Ph > 40 > 40 > 40 > 40 > 40
16 5-FU b 8.02 ± 2.35 37.51 ± 3.25 24.75 ± 5.80 11.35 ± 1.67 8.65 ± 0.81
  1. NCI-H460 human large cell lung cancer cell line, A549 human lung cancer cell line, NCI-H1975 human lung cancer cell line, HL-7702 human normal liver cells, MDCK Madin-Darby canine kidney cells
  2. aIC50 compound concentration required to inhibit tumor cell proliferation by 50%
  3. b5-Fluorouracil, used as a positive control