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1: Bioorg Med Chem Lett. 2004 Aug 2;14(15):4079-82.Click here to read Links

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

Miller ML, Roller EE, Wu X, Leece BA, Goldmacher VS, Chari RV, Ojima I.

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

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.

PMID: 15225730 [PubMed - indexed for MEDLINE]