Compounds R Cytotoxicity GI50 (µM)*
A2780 HCT-116
4a NHPh 38.7 ± 3.7 48.5 ± 3.0
4b NH-(m-Me)Ph 31.8 ± 5.9 >100
4c NH-(p-Me)Ph 44.6 ± 3.1 >100
4d NH-(o-Et)Ph 42.8 ± 4.8 >100
4e NH-(p-Et)Ph 52.1 ± 27.3 >100
4f NH-(o-CF3)Ph 45.0 ± 1.3 >100
4g NH-(p-CF3)Ph 40.6 ± 4.5 >100
4h NH-(o-MeO)Ph 63.5 ± 6.2 76.8 ± 4.7
4i NH-(p-MeO)Ph 46.7 ± 4.6 58.1 ± 5.6
4j NH-(p-F)Ph 29.1 ± 3.4 39.3 ± 2.9
4k NH-(o-Me-4-F)Ph 42.9 ± 5.8 >100
4l NHCH2Ph 73.9 ± 5.5 >100
4m NH-iPr 34.7 ± 2.4 59.2 ± 6.9
4n NH-nPr 55.5 ± 16.7 69.7 ± 5.2
4o NH(CH2)3N(CH3)2 31.7 ± 2.5 24.7 ± 3.4
4p NH-cyclohexyl 37.6 ± 8.8 50.1 ± 4.9
4q 1-morpholinyl 73.8 ± 6.7 56.4 ± 5.8
4r p-hydroxypipridinyl 68.7 ± 22.3 96.6 ± 10.7
4s p-methylpiperazinyl 45.9 ± 10.7 61.6 ± 8.5
4t p-acetylpiperazinyl 48.9 ± 8.2 >100
E7010 - 40.2 ± 2.1 64.4 ± 4.3
Table 1: The structures and anti-proliferative activity of 4a-t.