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Structure-activity relationship of analogues of compounds 4 and 12
| COMPOUND | R1 | R2 | Binding Affinities (IC50 ± SD, nM) | Cell Growth Inhibition (IC50 ± SD, nM) |
||
|---|---|---|---|---|---|---|
|
| ||||||
| Bcl-2 | Bcl-XL | Mcl-1 | H-146 | |||
| 5 | −OH | Et- | 2 ± 1.6 | 6.6 ± 2.3 | NT | 8.1 ± 3.5 |
| 28 | −OH | iPr- | 1.4 ± 0.5 | 4.8 ± 0.1 | NT | 3 ± 2.4 |
| 29 | −OH | Pr- | 10 ±4 | 8.2 ± 2.2 | NT | 42 ± 5 |
| 30 | −OH | Bu- | 23 ± 2 | 16 ± 2 | NT | 67 ± 5 |
| 31(BM-1075) | −NHSO2CH3 | Et- | 1.8 ± 0.3 | 7.0 ± 1.8 | > 2000 | 4.8 ± 0.9 |
| 32 (BM-1074) | −NHSO2CH3 | iPr- | 1.8 ± 0.2 | 6.9 ± 1.8 | > 2000 | 1.3 ± 0.3 |
NT = not tested
