Synthesis and biological evaluation of 1-deoxypaclitaxel analogues

Citation
Dgi. Kingston et al., Synthesis and biological evaluation of 1-deoxypaclitaxel analogues, J ORG CHEM, 64(6), 1999, pp. 1814-1822
Citations number
52
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
JOURNAL OF ORGANIC CHEMISTRY
ISSN journal
0022-3263 → ACNP
Volume
64
Issue
6
Year of publication
1999
Pages
1814 - 1822
Database
ISI
SICI code
0022-3263(19990319)64:6<1814:SABEO1>2.0.ZU;2-Z
Abstract
The naturally occurring taxoid baccatin VI has been converted to various 1- deoxypaclitaxel derivatives by selective deacylation followed by attachment of the C-13 side chain. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and seve ral analogues with activity comparable to that of paclitaxel were discovere d. It thus appears that the l-hydroxyl group is not necessary for the activ ity of paclitaxel.