2. Academic Validation
  3. Synthesis of taxoids with improved cytotoxicity and solubility for use in tumor-specific delivery

Synthesis of taxoids with improved cytotoxicity and solubility for use in tumor-specific delivery

  • J Med Chem. 2004 Sep 23;47(20):4802-5. doi: 10.1021/jm049705s.
Michael L Miller 1,  Elizabeth E Roller,  Robert Y Zhao,  Barbara A Leece,  Olga Ab,  Erkan Baloglu,  Victor S Goldmacher,  Ravi V J Chari
Affiliations

Affiliation

  • 1 ImmunoGen, Inc., 128 Sidney Street, Cambridge, Massachussetts 02139, USA.
PMID: 15369381 DOI: 10.1021/jm049705s
Abstract

To develop effective taxane-antibody immunoconjugates, we have prepared a series of modified taxanes that have both improved toxicity and solubility in aqueous systems as compared to paclitaxel (1a). These taxanes have been modified at either the C-10 or C-7 position and were found to be very cytotoxic against both normal and multi-drug-resistant (MDR) cells, as well as up to 30 times more soluble than paclitaxel in various buffer systems.

Figures
Products