SYNTHESIS AND BIOLOGICAL EVALUATION OF C-13 AMIDE-LINKED PACLITAXEL (TAXOL) ANALOGS

Citation
Sh. Chen et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF C-13 AMIDE-LINKED PACLITAXEL (TAXOL) ANALOGS, Journal of organic chemistry, 61(6), 1996, pp. 2065-2070
Citations number
46
Categorie Soggetti
Chemistry Inorganic & Nuclear
ISSN journal
00223263
Volume
61
Issue
6
Year of publication
1996
Pages
2065 - 2070
Database
ISI
SICI code
0022-3263(1996)61:6<2065:SABEOC>2.0.ZU;2-I
Abstract
Several C-13 amidopaclitaxel analogs have been synthesized during the course of our structure-activity relationship study at the C-13 positi on. These include 4-deacetyl-13-amidopaclitaxel (4), 13-amidopaclitaxe l 4-(methyl carbonate) derivatives (5a,b), and 13-amidopaclitaxel (6). None of these novel C-13 amidopaclitaxel analogs retain any activity in the tubulin polymerization assay or the in vitro cytotoxicity assay .