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Incorporation of a Michael acceptor enhances the antitumor activity of triterpenoic acids.

Abstract
Finding and developing drugs for the treatment of cancer has been challenging scientists for many decades, and using compounds of natural origin represents one of several strategies. Triterpenoic acids are a very promising class of secondary metabolites being able to induce apoptosis while their cytotoxicity is low. Therefore, derivatizations have to be conducted to improve cytotoxicity while retaining their ability to induce programmed cell death. The incorporation of a Michael acceptor into molecules resulted very often in drugs of improved cytotoxicity. Thus, in this study we synthesized and evaluated several Michael acceptor substituted compounds derived from glycyrrhetinic, ursolic, oleanolic and platanic acid. The influence of the presence of such a functional group onto the cytotoxicity was investigated in colorimetric sulforhodamine B assays employing several human cancer cell lines. EC50 values in the single-digit micromolar range were measured. Thus, the incorporation of a Michael acceptor unit into triterpenoic acids enhances the cytotoxicity of these compounds significantly.
AuthorsLucie Heller, Stefan Schwarz, Vincent Perl, Alexander Köwitsch, Bianka Siewert, René Csuk
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 101 Pg. 391-9 (Aug 28 2015) ISSN: 1768-3254 [Electronic] France
PMID26177446 (Publication Type: Journal Article)
CopyrightCopyright © 2015 Elsevier Masson SAS. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Triterpenes
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Conformation
  • Structure-Activity Relationship
  • Triterpenes (chemical synthesis, chemistry, pharmacology)
  • Tumor Cells, Cultured

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