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)|
|Number of pages||8|
|Journal||Biochemical and Biophysical Research Communications|
|State||Published - Apr 14 1982|
ASJC Scopus subject areas
- Molecular Biology
- Cell Biology