Table 3.
In vitro cytotoxicity of 3-amino substituted esters 26 and acids 27 and sodium salt 28
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---|---|---|---|---|
Compd | R1 | R2 | IC50 (μM)
|
|
DU145 | K562 | |||
26a | 2, 4, 6-(CH3O)3 | CH2 | 0.1 | 0.1 |
26b | 3, 4, 5-(CH3O)3 | CH2 | 75 | 30 |
26c | 2, 4, 6-(CH3O)3 | CH2CH2 | 1.5 | 1.0 |
26d | 2, 4, 6-(CH3O)3 | CH(CH3) | 0.75 | 0.2 |
26e | 2, 4, 6-(CH3O)3 | CF2 | 0.25 | 0.25 |
26f | 2, 4, 6-(CH3O)3 | CH(CF3) | 0.25 | 0.25 |
26g | 2, 4, 6-(CH3O)3 | C(CH3)2 | 2.5 | 0.80 |
26h | 2, 4, 6-(CH3O)3 | CH(C6H5) | 0.075 | 0.03 |
26i | 2, 4, 6-(CH3O)3 | CH(4-FC6H4) | 0.3 | 0.8 |
26j | 2, 4, 6-(CH3O)3 | CH(4-ClC6H4) | 0.4 | 0.2 |
26k | 2, 4, 6-(CH3O)3 | CH(4-BrC6H4) | 0.3 | 0.2 |
26l | 2, 4, 6-(CH3O)3 | CH(4-MeOC6H4) | 0.25 | 0.15 |
27a | 2, 4, 6-(CH3O)3 | CH2 | 0.075 | 0.0075 |
27b | 3, 4, 5-(CH3O)3 | CH2 | 5.0 | 3.0 |
27c | 2, 4, 6-(CH3O)3 | CH2CH2 | 5.0 | 5.0 |
27d | 2, 4, 6-(CH3O)3 | CH(CH3) | 0.025 | 0.015 |
27e | 2, 4, 6-(CH3O)3 | CF2 | 0.15 | 0.15 |
27f | 2, 4, 6-(CH3O)3 | CH(CF3) | 0.02 | 0.075 |
27g | 2, 4, 6-(CH3O)3 | C(CH3)2 | 0.15 | 0.0075 |
27h | 2, 4, 6-(CH3O)3 | CH(C6H5) | 0.02 | 0.015 |
27i | 2, 4, 6-(CH3O)3 | CH(4-FC6H4) | 0.15 | 0.08 |
27j | 2, 4, 6-(CH3O)3 | CH(4-ClC6H4) | 0.4 | 0.25 |
27k | 2, 4, 6-(CH3O)3 | CH(4-BrC6H4) | 0.3 | 0.2 |
27l | 2, 4, 6-(CH3O)3 | CH(4-OMeC6H4) | 0.1 | 0.015 |
28 | ON 01910 Na | 0.1 | 0.015 |