Proliferation inhibition (%)
Compound c-Srckinase Inhibition IC50 (µM)a HT-29 SK-OV-3 MCF-7
a1 12.9 70 42 NAc
a2 21 52 <30 NA
a3 NDb <30 <30 <30
a4 ND <30 NA <30
a5 >300 52 40 35
a6 ND 44 35 <30
a7 30.5 45 <30 35
a8 ND 62 70 69
a9 ND 4 <30 NA
a10 ND 66 52 <30
a11 ND 40 35 NA
a12 ND 62 35 NA
a13 27.5 37 <30 <30
a14 ND 33 <30 <30
a15 25.3 <30 <30 77
a16 36.1 52 47 45
a17 >300 45 <30 NA
a18 ND 52 <30 NA
a19 ND NA <30 <30
a20 35.2 67 62 50
a21 156.4 NA <30 <30
a22 21.2 76 68 35
a23 65.3 45 35 NA
a24 63.1 60 <30 76
a25 ND 48 <30 NA
a26 ND ND ND NDb
a27 97.2 67 48 <30
a28 ND 42 37 <30
a29 95.1 <30 <30 <30
a30 46.5 60 60 <30
a31 ND <30 <30 <30
a32 ND 40 32 <30
a33 ND NA <30 <30
a34 39.2 50 35 40
a36 46.2 55 38 <30
a37 178.9 33 <30 <30
a38 30.3 68 76 55
a39 >300 <30 <30 <30
a40 ND <30 NA <30
a41 69.1 <30 NA <30
a42 33.7 40 30> <30
aThe concentration that inhibited enzyme activity by 50%;
bNot determined;
c No activity. All data are average of triplicate experiments.
Table 3: The biological activity of compounds a1-42.