Synthesis and Interactions of 7-Deoxy-, 10-Deacetoxy, and 10-Deacetoxy-7-Deoxypaclitaxel with NCI/ADR-RES Cancer Cells and Bovine Brain Microvessel Endothelial Cells

Abstract

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 Pglycoprotein 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. ©2000 Elsevier Science Ltd. All rights reserved.