Development of enzymatically cleavable prodrugs derived from dendritic polyglycerol

Bioorg Med Chem Lett. 2009 Jul 15;19(14):3725-8. doi: 10.1016/j.bmcl.2009.05.058. Epub 2009 May 18.

Abstract

In this Letter we report the synthesis and in vitro studies of cleavable polymer-drug conjugates derived from dendritic polyglycerol and maleimide-bearing prodrugs of doxorubicin and methotrexate that are cleaved by cathepsin B. Cleavage properties and cytotoxicity of the new conjugates are presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cathepsin B / metabolism
  • Cell Line, Tumor
  • Dendrimers / chemistry
  • Doxorubicin / chemistry
  • Drug Carriers / chemical synthesis*
  • Drug Carriers / chemistry
  • Drug Screening Assays, Antitumor
  • Glycerol / chemistry*
  • Humans
  • Maleimides / chemistry
  • Methotrexate / chemistry
  • Polymers / chemistry*
  • Prodrugs / administration & dosage*
  • Prodrugs / chemistry
  • Prodrugs / pharmacology

Substances

  • Antineoplastic Agents
  • Dendrimers
  • Drug Carriers
  • Maleimides
  • Polymers
  • Prodrugs
  • maleimide
  • polyglycerol
  • Doxorubicin
  • Cathepsin B
  • Glycerol
  • Methotrexate