TABLE 2.
CXCR4/T-140-Fl inhibition data
| Starting amine | IC50 (μM)a |
|||
|---|---|---|---|---|
| Starting amine | Guanide | Biguanide | Phenylguanide | |
| Butanediamine | >200 | 50 | >200 | >200 |
| Hexanediamine | ≥200 | >200 | >200 | 150 (1), 20 (2) |
| Diethylenetriamine (DETA) | ≥200 | 50 | >200 | 15 (1), 6 (2) |
| Spermidine | >200 | 8 (2), 10 (3) | 65 (1-2) | 0.2 (2), 0.2 (3) |
| Spermine | 75 | 10 (2) | 4-8 (2) | 0.5 (3-4) |
| Trisethylaminomelamine (TEAM) | >200 | 20 | >200 (1) | 1.5 (3) |
| Trisbutylaminomelamine (TBAM) | ≥100 | 10 | >200 (1-2) | 6 (2), 20 (3) |
| Trishexylaminomelamine (THAM) | >200 | 2 | 45 (1-3) | >200 (2) |
| BEMA dimer | >200 | 50 | ND | 15 (1), 70 (2) |
| PAMAM GO | >200 | 4 | >50 (3-4) | 3 |
| DNT2300 | >200 | 8 | 7.5 (3-6) | 1.5 |
| DNT2200 | ≥200 | 15 | ≥200 (1-5) | 3.5 |
a
For comparison, NB325, assuming an average molecular weight of ∼1,000, has an IC50 of 10 μM. Numbers in parentheses indicate the number of groups added. ND, synthesis not done.