A novel arylethynyltriazole acyclonucleoside inhibits proliferation of drug-resistant pancreatic cancer cells

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5979-83. doi: 10.1016/j.bmcl.2010.08.093. Epub 2010 Aug 21.

Abstract

Novel arylethynyltriazole acyclonucleosides were synthesized and assessed for their anticancer activity on drug-resistant pancreatic cancer MiaPaCa-2 cells. One lead compound was found to have much more potent apoptosis-related antiproliferative effects than gemcitabine, the current first-line treatment for pancreatic cancer. Further investigations showed that this active compound did not inhibit DNA synthesis, which means that it does not resemble gemcitabine and may involve a different mechanism of action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / pharmacology
  • Drug Resistance, Neoplasm
  • Gemcitabine
  • Humans
  • Nucleosides / chemistry*
  • Nucleosides / pharmacology*
  • Pancreatic Neoplasms / drug therapy*
  • Triazoles / chemistry*
  • Triazoles / pharmacology*

Substances

  • Antineoplastic Agents
  • Nucleosides
  • Triazoles
  • Deoxycytidine
  • Gemcitabine