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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Investigation of Tubulin Polymerizing Agents: Synthesis of Substituted Cyclooctatrienes as a Possible Taxoid Framework

Author(s): A. Zand, P. Wagner, J. Song and J. Tischler

Volume 2, Issue 5, 2005

Page: [355 - 363] Pages: 9

DOI: 10.2174/1570180054405776

Price: $65


The taxane family of compounds has proven to be synthetically challenging targets. Using a novel [2+2] photocycloaddition reaction, several substituted cyclooctatrienes were synthesized and tested for tubulin polymerization activity. Elaboration of this methodology could allow the synthesis of a modified taxoid scaffold thereby permitting the efficient synthesis of paclitaxel analogs.

Keywords: paclitaxel, baccatin, taxoid framework, photocycloaddition, cyclooctatriene

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