| Literature DB >> 15863303 |
Ernst Binderup1, Fredrik Björkling, Pernille Vig Hjarnaa, Scilla Latini, Bodil Baltzer, Morten Carlsen, Lise Binderup.
Abstract
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.Entities:
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Year: 2005 PMID： 15863303 DOI： 10.1016/j.bmcl.2005.03.064
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823