Total synthesis of malformin C, an inhibitor of bleomycin-induced G2 arrest

J Antibiot (Tokyo). 2008 May;61(5):297-302. doi: 10.1038/ja.2008.42.

Abstract

Total synthesis of a fungal cyclic peptide, malformin C, recently rediscovered as a G2 checkpoint inhibitor was completed. Our synthesis involved a convergent approach with respect to a linear pentapeptide, cyclization, and oxidative disulfide formation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antineoplastic / antagonists & inhibitors*
  • Antibiotics, Antineoplastic / toxicity*
  • Bleomycin / antagonists & inhibitors*
  • Bleomycin / toxicity*
  • Cell Division / drug effects
  • Cyclization
  • DNA Damage / drug effects
  • Disulfides / chemistry
  • G2 Phase / drug effects*
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Oxidation-Reduction
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / pharmacology*
  • Spectrometry, Mass, Fast Atom Bombardment
  • Spectrophotometry, Infrared
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Antibiotics, Antineoplastic
  • Disulfides
  • Indicators and Reagents
  • Peptides, Cyclic
  • Bleomycin
  • malformins