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Synthesis of paclitaxel (docetaxel) / 2-deacetoxytaxinine J dimers
โ Scribed by Giovanni Appendino; Emanuela Belloro; Sven Jakupovic; Bruno Danieli; Jasmin Jakupovic; Ezio Bombardelli
- Book ID
- 104209393
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- French
- Weight
- 772 KB
- Volume
- 55
- Category
- Article
- ISSN
- 0040-4020
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โฆ Synopsis
Starting from taxenes available in multigram amounts from widespread ornamental yews (10deacetylbaccatin Ill (4) and 2'-deacetoxyaustrospicatine ( )), two dimeric taxoids (3a, 3b) with potential dual target specificity ([3-tubulin end P-gp) were synthesised. Both compounds lacked significant cytotoxicity, though 3b retained a strong activity in the tubulin depolimerisation assay.
๐ SIMILAR VOLUMES
Bifunctional, heterodimeric compounds were synthesized to test their ability to create polyvalent arrays between DNA and microtubules in cells. Each dimer was examined for the capacity to bind to microtubules and for cytotoxicity against MES-SA and MES-SA/Dx5 cell lines.