Table 2.
Yields and preliminary cell viability data for compounds 16a–n (Series IIIA) in MUTU-1 and DG-75 Burkitt lymphoma cell lines.
|
MUTU-1 Cell Viability % | DG-75 Cell Viability % | ||||
|---|---|---|---|---|---|---|
| Compound | Substitution | Yield (%) | 10 μM | 1 μM | 10 μM | 1 μM |
| 16a | R1=R2=R3=R4=R5=H | 30 | 1.4 | 10.3 | 1.1 | 1.1 |
| 16b | R1=R2=R3=R5=H, R4=Cl |
51 | 0.38 | 5.0 | 0.52 | 5.5 |
| 16c | R1=R2=R3=R5=H, R4=OCH3 |
70 | 1.1 | 0.19 | 2.1 | 28.4 |
| 16d | R1=Cl, R2=R3=R4=R5=H | 15 | 0.41 | 0.77 | 5.1 | 13.5 |
| 16e | R1=R2=R3=R5=H, R4=F |
27 | 1.4 | 0.07 | 2.3 | 35.4 |
| 16f | R1=R2=H, R3=R4=R5=OCH3 |
10 | 1.1 | 1.8 | 0.46 | 25.6 |
| 16g | R1=R2=R3=R5=H, R4=Br |
66 | 1.1 | 2.1 | 0.55 | 28.2 |
| 16h | R1=R2=R3=R5=H, R4=(C=O)OCH3 |
60 | 0.79 | 2.3 | 0.18 | 20.8 |
| 16i | R1=R2=R3=R5=H, R4=(C=O)C6H5 |
40 | 1.2 | 2.0 | 2.7 | 77.5 |
| 16j | R1=R2=R4=H, R3=R5=OCH3 |
63 | 5.4 | 4.2 | 0.16 | 33.5 |
| 16k | R1=R2=R4=R5=H, R3=Cl |
58 | 0.84 | 2.7 | 0 | 69.0 |
| 16l | R1=R3=R4=R5=H, R2=OH |
40 | 0.61 | 2.3 | 0 | 59.2 |
| 16m | R1=R2=R4=R5=H, R3=O(C=O)CH3 |
50 | 1.2 | 2.0 | 0 | 35.9 |
| 16n | R1=R2=R3=R5=H, R4=NH2 |
45 | 3.7 | 1.7 | 0.18 | 20.8 |
| Maprotiline 8 | - | - | 73.0 | 93.1 | 65.1 | 102.0 |
| Taxol | - | - | 9.8 | 30.4 | 9.9 | 48.8 |
Cell proliferation of MUTU-1 and DG-75 cells was determined with an alamarBlue assay (seeding density 1–5 × 104 cells/mL per well for 96-well plates). Compound concentrations of either 1 μM or 10 μM for 24 h (MUTU-1) or 48 h (DG-75) were used to treat the cells (in triplicate) with control wells containing vehicle ethanol (1% v/v). The mean value for three experiments is shown.