2. Academic Validation
  3. Synthesis and biological evaluation of a series of tangeretin-derived chalcones

Synthesis and biological evaluation of a series of tangeretin-derived chalcones

  • Bioorg Med Chem Lett. 2009 Jan 1;19(1):167-9. doi: 10.1016/j.bmcl.2008.10.126.
Jérôme Quintin 1,  Julie Desrivot,  Sylviane Thoret,  Patrick Le Menez,  Thierry Cresteil,  Guy Lewin
Affiliations

Affiliation

  • 1 Faculté de Pharmacie, Laboratoire de Pharmacognosie, Univ Paris-Sud 11, BIOCIS, UMR-8076 CNRS, Châtenay-Malabry Cedex, France.
PMID: 19013795 DOI: 10.1016/j.bmcl.2008.10.126
Abstract

A series of Chalcones polyoxygenated on the ring A (with pentamethoxy or 2'-hydroxy-3',4',5',6'-tetramethoxy substitution patterns) was synthesized from tangeretin, a natural Citrus flavonoid. These Chalcones were evaluated for their antiproliferative, activation of Apoptosis, inhibition of tubulin assembly and antileishmanial activities. Comparison with the reference analogous 3',4',5'-trimethoxylated Chalcones showed that such peroxygenated substitution patterns on the ring A were less beneficial to these activities.

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