Synthesis and Antitumor Activity of Novel C-7 Paclitaxel Ethers:  Discovery of BMS-184476

Autor: Altstadt, T. J., Fairchild, C. R., Golik, J., Johnston, K. A., Kadow, J. F., Lee, F. Y., Long, B. H., Rose, W. C., Vyas, D. M., Wong, H., Wu, M.-J., Wittman, M. D.
Zdroj: Journal of Medicinal Chemistry; December 2001, Vol. 44 Issue: 26 p4577-4583, 7p
Abstrakt: The preparation of C-7 paclitaxel ethers is described. Various substituted ethers were prepared via activation of the corresponding methylthiomethyl ether followed by alcohol addition. Variation of the C-7 ether group as well the 3‘ side chain position led to the discovery of a novel taxane, BMS-184476 (4), with preclinical antitumor activity superior to paclitaxel.
Databáze: Supplemental Index