New bis(pyridyl)methane derivatives from 4-hydroxy-2-pyridones: synthesis and antitumoral activity

Eur J Med Chem. 2003 Jan;38(1):37-47. doi: 10.1016/s0223-5234(02)00002-8.

Abstract

Bis(pyridyl)methane derivatives 5-40 were obtained from the reaction of 4-hydroxy-2-pyridones 3 and 4 with aldehydes. Compounds 5-40 were evaluated for cytotoxic activity against a panel of 60 human cancer cell lines by the National Cancer Institute and some of them demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10(-5) M level and in some case at 10(-7) M concentrations.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Methane / analogs & derivatives*
  • Methane / pharmacology
  • Models, Chemical
  • Molecular Structure
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Pyridones / chemistry*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyridines
  • Pyridones
  • 2,4-dihydroxypyridine
  • Methane