2. Academic Validation
  3. A novel aryl-hydrazide from the marine lichen Lichina pygmaea: isolation, synthesis of derivatives, and cytotoxicity assays

A novel aryl-hydrazide from the marine lichen Lichina pygmaea: isolation, synthesis of derivatives, and cytotoxicity assays

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4582-6. doi: 10.1016/j.bmcl.2010.06.013.
Catherine Roullier 1,  Marylène Chollet-Krugler,  Pierre van de Weghe,  Françoise Lohézic-Le Devehat,  Joël Boustie
Affiliations

Affiliation

  • 1 EA 4090 'Substances licheniques et photoprotection', Faculté des Sciences pharmaceutiques et Biologiques, Université Européenne de Bretagne, Université de Rennes, Rennes Cedex, France.
PMID: 20570625 DOI: 10.1016/j.bmcl.2010.06.013
Abstract

A new aryl-hydrazide l-glutamic acid derivative, pygmeine (3), was isolated from a methanolic extract of Lichina pygmaea, a marine Lichen. Synthetic derivatives obtained via a two-step coupling of l-glutamic acid with phenylhydrazine moieties were useful to elucidate the structure of 3 and to carry out biological assays. Thus, the cytotoxicity of the ortho-, meta-, and para-hydroxyl isomers along with their respective benzyl intermediates, and a natural methoxylated analog, were evaluated on murine and human melanoma cells (B16, A375). The para-hydroxyl isomer 6 was found to be the most active (IC(50)=1.6 microM) on B16 cells.

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