Synthesis of potent taxoids for tumor-specific delivery using monoclonal antibodies

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4079-82. doi: 10.1016/j.bmcl.2004.05.027.

Abstract

The targeted delivery of taxoids, in the form of taxane-antibody immunoconjugates, requires the preparation of taxoids containing moieties suitable for their conjugation to monoclonal antibodies. A series of taxoids incorporating a disulfide-containing linker at various positions of the taxoid framework have been prepared to investigate the most suitable position for conjugation. A second series of taxoids modified at the C-2 position aimed at increasing the potency of these taxanes has also been prepared.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antibodies, Monoclonal* / chemistry
  • Antibodies, Monoclonal* / toxicity*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival
  • Drug Delivery Systems
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Paclitaxel / toxicity
  • Structure-Activity Relationship
  • Taxoids / chemical synthesis*
  • Taxoids / toxicity*

Substances

  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Taxoids
  • Paclitaxel