Discovery of S-phase arresting agents derived from noscapine

J Med Chem. 2005 Apr 21;48(8):2756-8. doi: 10.1021/jm0494220.


Analogues of the natural product noscapine were synthesized, and their potential as antitumor agents were examined. The discovery of a novel regio- and stereoselective O-demethylation led to the synthesis of several O-alkylated analogues that induced an unexpected S-phase arrest of mammalian cells. Compound 4a was the most potent analogue inhibiting cell proliferation at an EC(50) of 1.9 microM.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Noscapine / analogs & derivatives*
  • Noscapine / chemical synthesis*
  • Noscapine / chemistry
  • Noscapine / pharmacology
  • S Phase / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship


  • Antineoplastic Agents
  • Noscapine