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Updated: Jun 14, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and In Vitro Evaluation of Taxol oxetane ring D precursors
Rüdiger Kaspera1, Jonathan L Cape, Juan A Faraldos
1Institute of Biological Chemistry, Washington State University, Pullman, WA 99164-6340.
Abstract:
A series of potential taxoid substrates was prepared in radiolabelled form to probe in vitro for the oxirane formation step and subsequent ring expansion step to the oxetane (ring D) presumably involved in the biosynthesis of the anticancer agent Taxol. None of the taxoid test substrates underwent transformation in cell-free systems from Taxus suggesting that these surrogates bore substitution patterns inappropriate for recognition or catalysis by the target enzymes, or that taxoid oxiranes and oxetanes arise by independent biosynthetic pathways.
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