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Synthesis, anti-cancer and anti-inflammatory activity of novel 2-substituted isoflavenes.

Abstract
Fifteen novel 2-substituted isoflavenes were synthesised via nucleophilic addition to isoflavylium salts. Twelve of the newly synthesised isoflavenes, along with the unsubstituted parent isoflavene, were tested in cell viability assays against the SHEP neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines. While the 2-substituted isoflavenes displayed a range of anti-proliferative activities, in most cases they were less active that the unsubstituted isoflavene (IC50=9.9 μM vs SHEP; IC50=33 μM vs MDA-MB-231). However, compound 7f, derived from the reaction between isoflavylium salt 5 and para-methoxyacetophenone, showed improved anti-proliferative activity against breast cancer cells (IC50=7.6 μM). Furthermore, compound 7f, as well as analogues 7a, 7c, 11d and 14, inhibited the production of interleukin-6 in LPS-activated RAW 264.7 cells.
AuthorsEleanor Eiffe, Eddy Pasquier, Maria Kavallaris, Cristan Herbert, David StC Black, Naresh Kumar
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 22 Issue 19 Pg. 5182-93 (Oct 01 2014) ISSN: 1464-3391 [Electronic] England
PMID25189689 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents
  • Flavonoids
  • Interleukin-6
  • Lipopolysaccharides
Topics
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (chemical synthesis, chemistry, pharmacology)
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Flavonoids (chemical synthesis, chemistry, pharmacology)
  • Humans
  • Interleukin-6 (antagonists & inhibitors, biosynthesis)
  • Lipopolysaccharides (antagonists & inhibitors, pharmacology)
  • Macrophages (drug effects, metabolism)
  • Mice
  • Molecular Structure
  • Structure-Activity Relationship

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