Synthesis, reactivity and biological evaluation of novel halogenated tripentones

Bioorg Med Chem. 2009 Nov 15;17(22):7783-8. doi: 10.1016/j.bmc.2009.09.027. Epub 2009 Sep 19.

Abstract

We describe herein the synthesis and the biological evaluation of a novel series of a potent anticancer agents: the tripentones. For the first time, a halogen atom was introduced in high yields on the pyrrole ring of the tricycle. This synthesis and the reactivity of the novel halogenated tripentones in metallo-catalysed cross-coupling reactions will be described in that article. Finally their influence on biological activity will be discussed.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cross-Linking Reagents / chemistry
  • Drug Evaluation, Preclinical
  • Humans
  • Hydrocarbons, Halogenated / chemical synthesis
  • Hydrocarbons, Halogenated / chemistry
  • Hydrocarbons, Halogenated / pharmacology*
  • Pyrrolizidine Alkaloids / chemical synthesis
  • Pyrrolizidine Alkaloids / chemistry
  • Pyrrolizidine Alkaloids / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Cross-Linking Reagents
  • Hydrocarbons, Halogenated
  • Pyrrolizidine Alkaloids