Table 2. SAR Study of Compounds 21–33.
No. | R4 | EC50(nM)a |
---|---|---|
21 | 2-Cl | 1143 ± 235 |
22 | 3-Cl | 257 ± 37 |
23 | 4-Cl | 66 ± 4.2 |
24 | 3-OH | 1821 ± 371 |
25 | 3-OMe | 57 ± 1.7 |
26 | 3-OEt | 110 ± 25 |
27 | 3-OPr | 69 ± 9.7 |
28 | 4-OMe | 94 ± 9.6 |
29 | 3-ethynyl | 4477 ± 1040 |
30 | 4-ethynyl | 817 ± 189 |
31 | 3-cyano | 4060 ± 477 |
32 | 4-cyano | 3489 ± 184 |
33b | 3,4-dimethoxy | 25 ± 0.57 |
EC50: cellular apoptosis inhibition in the U2OS_Bim cell line.
Compound A.