2. Academic Validation
  3. Synthesis and antitumor activity of novel C-7 paclitaxel ethers: discovery of BMS-184476

Synthesis and antitumor activity of novel C-7 paclitaxel ethers: discovery of BMS-184476

  • J Med Chem. 2001 Dec 20;44(26):4577-83. doi: 10.1021/jm0102607.
T J Altstadt 1,  C R Fairchild,  J Golik,  K A Johnston,  J F Kadow,  F Y Lee,  B H Long,  W C Rose,  D M Vyas,  H Wong,  M J Wu,  M D Wittman
Affiliations

Affiliation

  • 1 Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, P.O. Box 5100, Wallingford, Connecticut 06492-7660, USA.
PMID: 11741476 DOI: 10.1021/jm0102607
Abstract

The preparation of C-7 paclitaxel ethers is described. Various substituted ethers were prepared via activation of the corresponding methylthiomethyl ether followed by alcohol addition. Variation of the C-7 ether group as well the 3' side chain position led to the discovery of a novel taxane, BMS-184476 (4), with preclinical antitumor activity superior to paclitaxel.

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