Table 3.
Optimized compounds designed to accommodate the p2 pocket of Mcl-1 and Bfl-1with terminal R2 tert-butyl moiety.
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Compound | R1 | R2 | Mcl-1 Ki (μM) | Bfl-1 Ki (μM) |
23 | ![]() |
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0.073 ± 0.02 | 0.084 ± 0.04 |
24 | ![]() |
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0.094 ± 0.01 | 0.10 ± 0.02 |
25 | ![]() |
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0.29 ± 0.01 | 0.25 ± 0.05 |
26 | ![]() |
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0.074 ± 0.01 | 0.10 ± 0.04 |
27 | ![]() |
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0.95 ± 0.08 | 1.1 ± 0.4 |