Structure-activity study of cytotoxicity and microtubule assembly in vitro by taxol and related taxanes

Jerome Parness, David G.I. Kingston, Richard G. Powell, Carol Harracksingh, Susan B. Horwitz

Research output: Contribution to journalArticlepeer-review

116 Scopus citations

Abstract

Structure-activity relationships of natural and semisynthetic taxanes 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 and by inhibition of [3H]taxol binding to microtubule protein. Cytotoxicity and in vitro activity require both an intact taxane ring and ester side chain at position C-13. Addition of acetyl moieties at positions 2′ and 7 results in loss of in vitro activity but not cytotoxicity.

Original languageEnglish (US)
Pages (from-to)1082-1089
Number of pages8
JournalBiochemical and Biophysical Research Communications
Volume105
Issue number3
DOIs
StatePublished - Apr 14 1982

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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