Table 3.
Yields and preliminary cell viability data for compounds 17a–n, 18 (Series IIIB) in MUTU-1 and DG-75 Burkitt lymphoma cell lines a.
|
MUTU-1 Cell Viability % | DG-75 Cell Viability % | |||||
|---|---|---|---|---|---|---|---|
| Compound | n | Substitution | Yield (%) | 10 μM | 1 μM | 10 μM | 1 μM |
| 17a | 0 | R1=R3=R4=R5=R6=H, R2=CH3 | 88 | 68.6 | 79.8 | 88.9 | 78.3 |
| 17b | 0 | R1=R3=R4=R5=R6=H, R2=CH2CH3 | 82 | 83.4 | 92.6 | 99.9 | 96.4 |
| 17c | 0 | R1=R3=R4=R6=H, R5=Cl, R2=CH3 | 60 | 77.6 | 78.0 | 86.3 | 96.6 |
| 17d | 0 | R1=R3=R4=R6=H, R5=Cl, R2=CH2CH3 | 44 | 99.9 | 102.0 | 78.4 | 96.6 |
| 17e | 0 | R1=R3=R4=R6=H, R5=OCH3, R2=CH3 | 65 | 91.1 | 84.2 | 100.4 | 82.8 |
| 17f | 0 | R1=R3=R4=R6=H, R5=OCH3, R2=CH2CH3 | 54 | 84.5 | 86.5 | 85.1 | 91.4 |
| 17g | 0 | R1=Cl, R3=R4=R5=R6=H, R2=CH3 | 39 | 78.5 | 88.0 | 84.3 | 85.3 |
| 17h | 0 | R1=Cl, R3=R4=R5=R6=H, R2=CH2CH3 | 38 | 96.3 | 106.7 | 90.3 | 89.2 |
| 17i | 1 | R1=R3=R4=R5=R6=R2=H | 74 | 0.86 | 74.9 | 0.67 | 93.1 |
| 17j | 1 | R1=R3=R4=R5=R6=H, R2=CH3 | 62 | 85.6 | 94.6 | 87.9 | 103.6 |
| 17k | 1 | R1=R3=R4=R5=R6=H, R2=CH2CH3 | 50 | 94.0 | 80.4 | 96.0 | 74.8 |
| 17l | 1 | R1=R3=H, R4=R5=R6=OCH3, R2=CH3 | 45 | 77.3 | 66.8 | 82.1 | 81.9 |
| 17m | 1 | R1=R3=H, R4=R5=R6=OCH3, R2=CH2CH3 | 54 | 66.8 | 82.2 | 77.8 | 82.2 |
| 17n | 2 | R1=R3=R4=R5=R6=R2=H | 77 | 2.0 | 2.8 | 0.070 | 19.9 |
| 18 | 0 | - | 68 | 13.2 | 75.0 | 13.2 | 87.3 |
|
Maprotiline
8 |
- | - | - | 73.0 | 93.1 | 65.1 | 102.0 |
| Taxol | - | - | - | 9.8 | 30.4 | 9.9 | 48.8 |
a 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.