1. Academic Validation
  2. Synthesis of potent taxoids for tumor-specific delivery using monoclonal antibodies

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.
Michael L Miller 1 Elizabeth E Roller Xinyaun Wu Barbara A Leece Victor S Goldmacher Ravi V J Chari Iwao Ojima
Affiliations

Affiliation

  • 1 ImmunoGen, Inc., 128 Sidney Street, Cambridge, MA 02139, USA. michael.miller@immunogen.com
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.

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