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

Starting from taxanes available in multigram amounts from widespread ornamental yews (10-deacetylbaccatin III ( 4) and 2′-deacetoxyaustrospicatine ( 5)), two dimeric taxoids ( 3a, 3b) with potential dual target specificity (β-tubulin and P-gp) were synthesised. Both compounds lacked significant cyto...

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Bibliographic Details
Published in:Tetrahedron 1999-05, Vol.55 (21), p.6567-6576
Main Authors: Appendino, Giovanni, Belloro, Emanuela, Jakupovic, Sven, Danieli, Bruno, Jakupovic, Jasmin, Bombardelli, Ezio
Format: Article
Language:English
Subjects:
Antitumour compounds
Dimers
Taxoids
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Summary:Starting from taxanes available in multigram amounts from widespread ornamental yews (10-deacetylbaccatin III ( 4) and 2′-deacetoxyaustrospicatine ( 5)), two dimeric taxoids ( 3a, 3b) with potential dual target specificity (β-tubulin and P-gp) were synthesised. Both compounds lacked significant cytotoxicity, though 3b retained a strong activity in the tubulin depolimerisation assay. Starting from taxanes available in multigram amounts from widespread ornamental yews, two dimeric taxoids ( 3a,3b) with potential dual target specificity (β-tubulin and P-gp) were synthesised. Both compounds lacked significant cytotoxicity, though 3b retained a strong activity in the tubulin test.
ISSN:0040-4020
1464-5416
DOI:10.1016/S0040-4020(99)00290-2