Tenovin SAR Studies Aimed at Increasing Water Solubility
| ID |
 |
p53 Increasea | K40Ac Tubulin Increaseb | SirT2 Inhibitionc | |
|---|---|---|---|---|---|
| R1 | R2 | ||||
| Tenovin-1 | tBu | NHCOCH3 | + | + | + |
| Tenovin-2 | tBu | NHCOCH(CH3)2 | + | + | + |
| Tenovin-3 | tBu | NH2 | + | + | + |
| Tenovin-4 | N3 | NHCOCH3 | − | − | − |
| Tenovin-5 | tBu | NHCOPh | + | + | + |
| Tenovin-6 | tBu | NHCO(CH2)4NMe2.HCl | + | + | + |
- a Ability to increase p53 levels was determined in MCF-7 cells treated for 6 hr at 10 μM.
- b Ability to increase K40 Ac-tubulin levels was determined in H1299 cells treated
- c SirT2 inhibition assessed using a compound concentration of 10 or 30 μM depending on the compound's solubility in the assay buffer.