Synthesis and antiproliferative activity of 2-triazenothiophenes

Anticancer Res. 1999 May-Jun;19(3A):2127-31.

Abstract

A series of 2-triazenothiophene derivatives was prepared and tested to evaluate their biological activity. Two compounds inhibited the proliferation of leukemia, lymphoma and solid tumor-derived cell lines at micromolar concentrations, whereas none of the compounds were active against HIV-1. Compound 3c inhibited DNA, RNA and protein synthesis, and was also effective against KB cells resistant to etoposide and vincristine. The compounds were inactive against fungi and bacteria.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents
  • Anti-HIV Agents / pharmacology
  • Anti-Infective Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects
  • Carcinoma / pathology
  • Cytopathogenic Effect, Viral / drug effects
  • Drug Evaluation, Preclinical
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Fungi / drug effects
  • HIV-1 / drug effects
  • HeLa Cells / drug effects
  • Humans
  • KB Cells / drug effects
  • Leukemia / pathology
  • Lymphoma / pathology
  • Melanoma / pathology
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis
  • Thiophenes / pharmacology*
  • Triazenes / chemical synthesis
  • Triazenes / pharmacology*
  • Tumor Cells, Cultured / drug effects

Substances

  • Anti-Bacterial Agents
  • Anti-HIV Agents
  • Anti-Infective Agents
  • Antineoplastic Agents
  • Thiophenes
  • Triazenes