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. 2017 Jul 5;10(3):62. doi: 10.3390/ph10030062

Table 1.

NCI-60 single dose results for 3,4-diaryl-5-aminopyrazoles.

graphic file with name pharmaceuticals-10-00062-i001.jpg

No. Substituents NSC No. Mean (%) Selected Cells (% Growth) Renal Cells Mean (%) Regioisomer Correlation
HOP-92 SNB-75 CAKI-1 UO-31
X R
32 CH H 776698 95.8 89.6 91.0 103.3 71.5 94.9
33 CH CH3 776695 95.4 - 77.9 100.4 66.4 93.4
34 CH (CH2)5CN 776696 96.8 69.1 96.3 106.4 77.3 94.9
35 N H 776697 98.4 83.4 94.0 101.9 86.1 97.3
R1 R2
40 NH2 H 763892 79.8 47.9 34.4 48.9 49.6 76.4 0.791
41 -NHCONHCO- 763893 101.5 87.7 67.2 89.8 94.2 100.7 0.366
42 -NC(CF3)CHC(CF3)- 763894 95.4 - 73.2 82.3 71.2 92.6 0.632
44 NH2 COCH3 763896 76.6 - 8.5 39.7 33.1 68.7 0.475
45 NH2 CSNHCH3 763895 78.6 - 26.5 34.1 35.9 71.1 0.805
R3 R4
46 NH2 H 754616 75.1 30.9 38.1 50.0 51.7 70.8 0.791
47 -NHCONHCO- 754617 104.3 53.5 99.7 118.4 94.8 101.4 0.366
48 -NC(CF3)CHC(CF3)- 754618 94.0 -3.1 67.2 - 73.7 92.5 0.632
49 NH2 COCH3 763899 104.2 86.4 101.9 81.0 92.8 97.6 0.475
50 NH2 CSNHCH3 763898 66.5 - 39.7 18.2 25.3 61.5 0.805
R5 R6
51 NH2 H 763905 70.6 - 4.8 18.8 24.6 65.0
52 -NHCONHCO- 763910 75.1 - 47.2 52.9 43.9 80.3
53 -NC(CF3)CHC(CF3)- 763909 92.9 48.6 56.3 55.2 61.4 87.5
54 NH2 COCH3 763906 69.4 - 40.3 18.1 23.7 60.6
55 NH2 CSNHCH3 763907 59.3 0.3 27.8 16.3 17.9 53.2