Design and synthesis of ( E )-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

The compound AK34, derived from Tripolin A, shows a pronounced inhibitory effect on Aurora A kinase with high affinity (IC 50 = 1.68 μM, K D = 216 nM). SAR and molecular docking indicate that these ( E )-3-benzylideneindolin-2-one derivatives tend to act on an allosteric Site 3 predicted by AlloReverse.