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 language | English (US) |
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Pages (from-to) | 1082-1089 |
Number of pages | 8 |
Journal | Biochemical and Biophysical Research Communications |
Volume | 105 |
Issue number | 3 |
DOIs | |
State | Published - Apr 14 1982 |
ASJC Scopus subject areas
- Biophysics
- Biochemistry
- Molecular Biology
- Cell Biology