Synthesis and anti-cancer activity of C-ring-functionalized prodigiosin analogues

J Med Chem. 2007 Apr 5;50(7):1528-36. doi: 10.1021/jm061088f. Epub 2007 Mar 10.

Abstract

Prodigiosin is the parent member of the 4-methoxypyrrolyldipyrromethene family of natural products and is known for its anti-cancer activity. A new series of analogues was synthesized, incorporating pendent functional esters and beta-carbonyl substituents on the C-ring. The beta-carbonyl group allowed for the facile isolation of the prodigiosenes, and the pendent esters allow for further derivatization. The novel prodigiosenes generally retain the anti-cancer activity of prodigiosin in 60 human cell lines derived from nine cancer cell types, with neither the conjugated beta-carbonyl group, as either ketone or ester, nor the pendent ester significantly reducing the anti-cancer activity of the core skeleton.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Prodigiosin / analogs & derivatives*
  • Prodigiosin / chemical synthesis*
  • Prodigiosin / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • ethyl 5-((3-methoxy-5-(1H-pyrrol-2-yl)-1H-pyrrol-2-yl)methylene)-2,4-dimethyl-5H-pyrrole-3-carboxylate
  • Prodigiosin