Synthesis of paclitaxel (Docetaxel)/2-deacetoxytaxinine J dimers

Authors
Appendino, G Belloro, E Jakupovic, S Danieli, B Jakupovic, J Bombardelli, E
Citation
G. Appendino et al., Synthesis of paclitaxel (Docetaxel)/2-deacetoxytaxinine J dimers, TETRAHEDRON, 55(21), 1999, pp. 6567-6576
Citations number
37
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON
ISSN journal
00404020 → ACNP
Volume
55
Issue
21
Year of publication
1999
Pages
6567 - 6576
Database
ISI
SICI code
0040-4020(19990521)55:21<6567:SOP(JD>2.0.ZU;2-0
Abstract
Starting from taxanes available in multigram amounts from widespread orname ntal yews (10-deacetylbaccatin III (4) and 2'-deacetoxyaustrospicatine (5)) , two dimeric taxoids (3a, 3b) with potential dual target specificity (beta -tubulin and P-gp) were synthesised. Both compounds lacked significant cyto toxicity, though 3b retained a strong activity in the tubulin depolimerisat ion assay. (C) 1999 Elsevier Science Ltd. All rights reserved.