Table 9.
Yields and preliminary cell viability data for compounds 23a–k (Series VII) in MUTU-1 and DG-75 Burkitt lymphoma cell lines a.
|
MUTU-1 Cell Viability % | DG-75 Cell Viability % | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Compound | X | Y | R1 | R2 | R3 | Yield (%) | 10 μM | 1 μM | 10 μM | 1 μM |
| 23a | O | C | H | CN | H | 74 | 82.6 | 82.7 | 75.8 | 89.0 |
| 23b | NH | C | H | CN | H | 38 | 79.4 | 79.4 | 54.1 | 101.1 |
| 23c | N(C6H5) | C | H | CN | H | 20 | 74.1 | 90.7 | 89.1 | 94.4 |
| 23d | O | C | H | CN | CN | 15 | 82.7 | 99.8 | 95.7 | 103.1 |
| 23e | NH | C | H | CN | CN | 42 | 83.6 | 82.9 | 98.7 | 85.7 |
| 23f | N(C6H5) | C | H | CN | CN | 44 | 71.8 | 78.9 | 81.6 | 82.0 |
| 23g | NH | N | H | NH2 | H | 63 | 100.9 | 95.2 | 55.0 | 78.1 |
| 23h | N(C6H5) | N | H | NH2 | H | 54 | 78.0 | 91.1 | 87.4 | 85.8 |
| 23i | NH | N | Cl | NH2 | H | 34 | 106.2 | 102.1 | 18.9 | 85.8 |
| 23j | NH | N | H | OH | H | 43 | 87.6 | 92.8 | 63.9 | 69.1 |
| 23k | N(C6H5) | N | H | OH | H | 66 | 83.9 | 96.9 | 74.1 | 81.7 |
| 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.