A novel bitriazolyl acyclonucleoside endowed with dual antiproliferative and immunomodulatory activity

J Med Chem. 2012 Jun 14;55(11):5642-6. doi: 10.1021/jm300534u. Epub 2012 May 21.

Abstract

A novel bitriazolyl acyclonucleoside was discovered to exhibit powerful antiproliferative effects on different cancer cell lines through caspase-dependent apoptosis and at the same time stimulate the immune response in dendritic cells via Toll-like receptor 7 (TLR7) signaling. This promising compound with dual anticancer and immunomodulatory activity may represent a new generation of highly efficacious drug candidates for use in cancer therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Dendritic Cells / drug effects
  • Dendritic Cells / immunology
  • Dendritic Cells / metabolism
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Humans
  • Immunologic Factors / chemical synthesis*
  • Immunologic Factors / chemistry
  • Immunologic Factors / pharmacology
  • Interleukin-6 / biosynthesis
  • Membrane Glycoproteins / genetics
  • Membrane Glycoproteins / metabolism
  • Mice
  • Mice, Knockout
  • Nucleosides / chemical synthesis*
  • Nucleosides / chemistry
  • Nucleosides / pharmacology
  • Structure-Activity Relationship
  • Toll-Like Receptor 7 / genetics
  • Toll-Like Receptor 7 / metabolism
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Antineoplastic Agents
  • Immunologic Factors
  • Interleukin-6
  • Membrane Glycoproteins
  • Nucleosides
  • Tlr7 protein, mouse
  • Toll-Like Receptor 7
  • Triazoles