Table 2.
Compound | Linkers | Methylenes per repeat | Therapeutic index
|
|||
---|---|---|---|---|---|---|
VII-IIIBa,b | VII-BaLa | CFI-IIIBc | CAI-IIIBc | |||
PEB | 2-2 | 4 | 14 | ND | ND | ND |
PEHMB | 2-6 | 8 | 78 | 53 | 14 | 86 |
PTMB | 4-4 | 8 | 17 | ND | ND | ND |
PPHMB | 3-6 | 9 | 72 | 1 | 3 | 77 |
PBHMB | 4-6 | 10 | 31 | 17 | 6 | 50 |
PEOMB | 2-8 | 10 | 62 | 52 | 5 | 59 |
PHMB | 6-6 | 12 | 10 | ND | ND | ND |
PEHMBd | 2-6 | 8 | 7000 | 266 | ND | ND |
ND: not determined.
An in vitro TI was calculated for each compound by dividing its CC50 value (2-h exposure) by the IC50 value determined in the VII-IIIB or VII-BaL assay.
In vitro TIs for PEB, PTMB, and PHMB were calculated using data from previous studies [16].
An in vitro TI was calculated for each compound by dividing its CC50 value (10-min exposure) by the IC50 value determined in the CFI-IIIB or CAI-IIIB assay.
PEHMB (2-6) (also known as NB325) produced using an improved synthesis protocol and partial purification.