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 language | English (US) |
|---|---|
| Pages (from-to) | 329-336 |
| Number of pages | 8 |
| Journal | Biochemical and Biophysical Research Communications |
| Volume | 124 |
| Issue number | 2 |
| DOIs | |
| State | Published - Oct 30 1984 |
ASJC Scopus subject areas
- Biophysics
- Biochemistry
- Molecular Biology
- Cell Biology
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Mellado, W., Magri, N. F., Kingston, D. G. I., Garcia-Arenas, R., Orr, G. A., & Horwitz, S. B. (1984). Preparation and biological activity of taxol acetates. Biochemical and Biophysical Research Communications, 124(2), 329-336. https://doi.org/10.1016/0006-291X(84)91557-2