Table 2. Biological Activity and Physicochemical Properties of Truncated Analoguesa.

| ID | R | 7 | L.inf pEC50 | PMM pCC50 | SI | aq. sol.b | HLM clintc | RH clintd | LLEe |
|---|---|---|---|---|---|---|---|---|---|
| 7b | NH2 | OMe | 4.5 | 4.2 | 2 | 290 | 120 | 7.1 | 4.1 |
| 11a | H | H | 4.3 | 4.2 | 1 | 828 | 130 | 140 | 2.6 |
| 11b | H | OMe | 4.6 | 4.2 | 3 | 723 | >300 | 53 | 2.4 |
| 12 | Cl | OMe | 4.8 | 4.5 | 2 | 562 | >300 | 17 | 2.2 |
nt, not tested.
Thermodynamic aqueous solubility μM.
μL/min/mg protein.
μL/min/106 cells.
LLE = pEC50 – LogD7.4.