Synthesis of heterobicyclic nitrogen systems bearing the 1,2,4-triazine moiety as anti-HIV and anticancer drugs, part III

Pharmazie. 2001 May;56(5):376-83.

Abstract

Some new fused heterobicyclic nitrogen systems such as 1,2,4-triazino[3,4-b] [1,3,4] thiadiazolones/thiadiazinones 4-15 and the related compounds 16-21 have been synthesized from treatment of 4-amino-3-mercapto-6-substituted-1,2,4-triazin-5-ones 1 with bifunctional oxygen and halogen compounds via heterocyclization reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant anti-HIV and anticancer activities were observed in vitro for some members of the series, compounds 1e, 4e, 4f, 5, 6 and 16 showing a significant activity in Leukemia, Lung, Breast and CNS anticancer evaluation.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Drug Screening Assays, Antitumor
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Quantitative Structure-Activity Relationship
  • Spectrophotometry, Infrared
  • Spectrophotometry, Ultraviolet
  • Triazines / chemical synthesis*
  • Triazines / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Anti-HIV Agents
  • Antineoplastic Agents
  • Heterocyclic Compounds
  • Triazines