Cathepsin B-sensitive dipeptide prodrugs. 2. Models of anticancer drugs paclitaxel (Taxol), mitomycin C and doxorubicin

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3347-52. doi: 10.1016/s0960-894x(98)00610-6.

Abstract

Substrates containing doxorubicin (DOX), paclitaxel (taxol), and mitomycin C (MMC) attached to the cathepsin B-sensitive dipeptide Phe-Lys via a self-immolative spacer were prepared as model compounds for internalizing anticancer immunoconjugates. Cathepsin B-mediated release rates of free drug, rat liver lysosomal susceptibility and human plasma stability were measured for each.

MeSH terms

  • Animals
  • Cathepsin B / metabolism*
  • Dipeptides / chemical synthesis*
  • Dipeptides / chemistry
  • Dipeptides / metabolism
  • Doxorubicin / chemical synthesis*
  • Drug Carriers
  • Drug Stability
  • Humans
  • Mitomycin / chemical synthesis*
  • Mitomycin / chemistry
  • Mitomycin / metabolism
  • Paclitaxel / chemical synthesis*
  • Paclitaxel / chemistry
  • Paclitaxel / metabolism
  • Prodrugs / chemical synthesis*
  • Prodrugs / chemistry
  • Prodrugs / metabolism
  • Rats

Substances

  • Dipeptides
  • Drug Carriers
  • Prodrugs
  • Mitomycin
  • Doxorubicin
  • Cathepsin B
  • Paclitaxel