M. Xue et al., Structure-activity relationships study at the 3 '-N position of paclitaxel. Part 2: Synthesis and biological evaluation of 3 '-N-thiourea- and 3 '-N-thiocarbamate-bearing paclitaxel analogues, BIOORG MED, 10(12), 2000, pp. 1327-1331
The syntheses and preliminary biological evaluation of 3'-N-thiocarbamate-
and 3'-N'-thiourea-bearing paclitaxel analogues, 4a-f and 5a-e, are describ
ed. 3'-N-thiocarbamates 4a-e were found to be more potent than paclitaxel i
n both the tubulin polymerization assay and the in vitro cytotoxicity assay
. Several derivatives of this class such as 4c, 4d, and 4e also exhibited s
ome in vivo activity. (C) 2000 Elsevier Science Ltd. All rights reserved.