2. Academic Validation
  3. A macromolecular prodrug of doxorubicin conjugated to a biodegradable cyclotriphosphazene bearing a tetrapeptide

A macromolecular prodrug of doxorubicin conjugated to a biodegradable cyclotriphosphazene bearing a tetrapeptide

  • Bioorg Med Chem Lett. 2005 Aug 1;15(15):3576-9. doi: 10.1016/j.bmcl.2005.05.057.
Jin Kyu Kim 1,  Udaya S Toti,  Rita Song,  Youn Soo Sohn
Affiliations

Affiliation

  • 1 Department of Chemistry, Division of Nano Science, Ewha Womans University, Seoul 120-750, South Korea.
PMID: 15982876 DOI: 10.1016/j.bmcl.2005.05.057
Abstract

A new biodegradable water-soluble phosphazene trimer-doxorubicin conjugate was synthesized, in which equimolar hydrophilic methoxy-poly(ethylene glycol) with a molecular weight of 350 (MPEG350) and a tumor-specific tetrapeptide (Gly-Phe-Leu-Gly) were grafted to cyclotriphosphazene. The present conjugate exhibited cytotoxicity lower than that of free doxorubicin (IC50=0.10 microM) but a reasonably higher in vitro cytotoxicity (IC50=1.1 microM) against the leukemia L1210 cell line probably due to its enzymatically controlled release.

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