7-Deoxypaclitaxel, 10-deacetoxypaclitaxel and 10-deacetoxy-7- deoxypaclitaxel were prepared and evaluated for their ability to promote assembly of tubulin into microtubules, their cytotoxicity against NCI/ADR-RES cells and for their interactions with P-glycoprotein in bovine brain microvessel endothelial cells. The three compounds were essentially equivalent to paclitaxel in cytotoxicity against NCI/ADR-RES cells. They also appeared to interact with P-glycoprotein in the endothelial cells with the two 10-deacetoxy compounds having less interaction than paclitaxel and 7-deoxypaclitaxel.
Bibliographical noteFunding Information:
The authors thank the National Cancer Institute for financial support of this research (NIH CA82801) and Tapestry Pharmaceuticals (Boulder, CO) for a generous gift of paclitaxel.
- Bovine brain microvessel endothelial cells
- P-glycoprotein interaction