Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378915 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
To overcome pharmacokinetic and solubility problems observed in early clinical trials with the potent anticancer compound CHS828, we synthesised a series of prodrugs with improved properties. The best compound obtained was EB1627, with a tetraethyleneglycol moiety attached to the parent drug via a carbonate linkage. This compound was found soluble enough to be given i.v. and the drug was rapidly released in vivo exerting a very potent inhibitory activity alone and in combination with known cytostatics (etoposide) in animal models in vivo.
Graphical abstractThe preparation and biological activity of (EB1627), a soluble pro-drug of the potent of anticancer cyanoguanidine CHS828, is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide