Preparation and biological activity of taxol acetates

Wilfredo Mellado, Neal F. Magri, David G.I. Kingston, Renee Garcia-Arenas, George A. Orr, Susan Band Horwitz

Research output: Contribution to journalArticle

95 Scopus citations

Abstract

Synthesis and biological activity of 2′-acetyltaxol and 7-acetyltaxol are reported. Activity is measured in vivo by cytotoxicity toward the macrophage-like cell line J774.2, and in vitro by promotion of microtubule assembly in the absence of exogenous GTP. Addition of an acetyl moiety at C-2′ results in loss of in vitro activity but not cytotoxicity. The properties of 7-acetyltaxol are similar to those of taxol in its effects on cell replication and on in vitro microtubule polymerization. Therefore a free hydroxyl group at C-7 is not required for in vitro activity and this position is available for structural modifications.

Original languageEnglish (US)
Pages (from-to)329-336
Number of pages8
JournalBiochemical and Biophysical Research Communications
Volume124
Issue number2
DOIs
StatePublished - Oct 30 1984

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

Fingerprint Dive into the research topics of 'Preparation and biological activity of taxol acetates'. Together they form a unique fingerprint.

  • Cite this