TABLE 1.
In the chemical structure, Ac represents acetyl.
Fully extended length (in angstroms) (number of bonds) × 1.2 Å (average bond contribution).
The decrease in activity observed with the longer dimers (dimers 11 and 12) may partially reflect the entropic penalty required to uncoil the polyethylene glycol linker.
Average EC50 (±standard deviations) are provided for assays performed three or more times (number in parentheses). No evidence of cytotoxicity was observed at concentrations up to 100 ng/ml for compounds 4 to 12 and at concentrations up to 1,000 ng/ml for compounds 2 and 2a.