Semi-Synthesis and In-Vitro Anticancer Evaluation of Derivatives of a New Microtubule Poison with a Taxol-Like Mechanism

Abstract

Taccaldnolides are structurally unusual steroid derivatives with microtubule-stabilizing, i.e. Tasol-like activity. The aim of the work is definition of a minimal structural motif that on the one had simplifies' the structure but improves of at least retains potency as an antimitotic. Taccalonolide E, a minor compound found in Tacca chantrieri, has been found to be a more potent cytotoxin that taccalonolide A. The two compounds differ by additional oxygenation in ring C of taccalonolide A. We therefore focused on removing the two acetoxy functions in this ring of taccalonolide A by means of biocatalysis. This approach has so far not proven productive. The use of enzymes immobilized on a suitable solid support is now being pursued with the expectation that improved recovery will be observed. Functional group removals at other sites in taccalonolide A by chemical means are being pursued.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2003
Accession Number
ADA419388

Entities

People

  • Thomas U. Hemscheidt

Organizations

  • University of HawaiĘ»i System

Tags

DTIC Thesaurus Topics

  • Biomedical Research
  • Classification
  • Cytoskeleton
  • Electronic Mail
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  • Maryland
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  • Universities

Fields of Study

  • Chemistry

Readers

  • Electrochemical Surface Science
  • Molecular and Cellular Biochemistry
  • Oncology (Cancer Research).