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. Author manuscript; available in PMC: 2014 Jul 11.
Published in final edited form as: J Med Chem. 2013 Jun 25;56(13):10.1021/jm400575x. doi: 10.1021/jm400575x

Table 1.

In vitro Cytotoxicity of (E)-N-Aryl-2-arylethenesulfonamides (6)

graphic file with name nihms492340u1.jpg
Compd R R1 IC50(μM)a
DU145 K562
6a H H 10 10
6b 4-Cl H 20 20
6c 4-F 4-Br 10 10
6d 4-F 4-OCH3 10 10
6e 4-OCH3 2-OCH3 5 5
6f 4-OCH3 4-OCH3 5 5
6g 4-OCH3 2,4-(OCH3)2 15 15
6h 4-OCH3 2,6-(OCH3)2 0.375 5
6i 4-OCH3 2,4,6-(OCH3)3 0.2 0.075
6j 4-OCH3 3,4,5-(OCH3)3 35 35
6k 2,4,6-(OCH3)3 4-OCH3 7.5 2.5
6l 4-OCH3 2,6-(OCH3)2,4-OH 10 10
6m 4-OCH3 2,4,6-F3 75 15
6n 4-OCH3 2,3,4,5,6-F5 10 5.0
6o 3-F,4-OCH3 2,4,6-(OCH3)3 0.2 0.075
6p 3-OH,4-OCH3 2,4,6-(OCH3)3 0.03 0.015
6q 3-OCOCH2C(CH3)2-C6H(CH3)2O2, 4-OCH3 2,4,6-(OCH3)3 0.009 0.008
6r 3-OPO(ONa)2,4-OCH3 2,4,6-(OCH3)3 0.04 0.0075
6s 3-NO2,4-OCH3 2,4,6-(OCH3)3 2.5 1.0
6t 3-NH2,4-OCH3 2,4,6-(OCH3)3 0.005 0.003
6u 3-NO2,4-OCH3 3,4,5-(OCH3)3 75 75
6v 3-NH2,4-OCH3 3,4,5-(OCH3)3 35 15
6w 3-NO2,4-OCH3 2,6-(OCH3)2,4-O(CH2)3COOH 100 100
6x 3-NH2,4-OCH3 2,6-(OCH3)2,4-O(CH2)3COOH 10 10
6y 3-OH,4-OCH3 2,6-(OCH3)2,4-O(CH2)3COOH 10 10
6z 3-NO2,4-F 2,4,6-(OCH3)3 100 75
6aa 3-NH2,4-F 2,4,6-(OCH3)3 10 5
6ab 3,5-(NO2)2,4-OCH3 2,4,6-(OCH3)3 10 10
6ac 3,5-(NH2)2,4-OCH3 2,4,6-(OCH3)3 2.5 7.5
6ad 3-F,4-OCH3 4-OCH3 5 1
6ae 3-F,4-OCH3 2,3,4,5,6-F5 10 10
6af 3-NO2,4-OCH3 2,3,4,5,6-F5 100 100
6ag 3-NH2,4-OCH3 2,3,4,5,6-F5 75 75
6ah 2,3,4,5,6-F5 3-NO2,4-OCH3 100 75
6ai 2,3,4,5,6-F5 3-NH2,4-OCH3 35 35
6aj 2,3,4,5,6-F5 2,3,4,5,6-F5 35 35
a

IC50 values are the compound concentrations (μM) required to inhibit cell proliferation by 50% of tumor cells following 96 h treatment with the tested compound; values represent the mean SD from the dose response curves of two independent experiments and are within 5–10%.