Activities of migrastatin analogs reported in ref. 18.
| Compound name | 4T1 tumor cell migration (IC50) | Stability (t1/2, mouse plasma) |
|---|---|---|
| Migrastatin | 29 μM | >60 min |
| 2,3-Dihydromigrastatin | 10 μM | >60 min |
| N-methyl 2,3-dihydromigrastatin | 7.0 μM | >60 min |
| Migrastatin core | 22 nM | 20 min |
| Macrolactone | 24 nM | <5 min |
| Acetylated macrolactone | 192 nM | NA |
| Oxidized macrolactone | 223 nM | NA |
| Hydrolized core | 378 nM | NA |
| Macrolactam | 255 nM | >60 min |
| Macroketone | 100 nM | >60 min |
| (S)-isopropyl macrolactone | 227 μM | >60 min |
| (R)-isopropyl macrolactone | 146 μM | >60 min |
| Macrocyclic secondary alcohol | 8.9 μM | NA |
| Macrocyclic tertiary alcohol | 3.1 μM | NA |
| Macrocyclic CF3-alcohol | 101 nM | NA |