Design and synthesis of novel 1,2,3-triazole-pyrimidine-urea hybrids as potential anticancer agents

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1124-8. doi: 10.1016/j.bmcl.2014.12.087. Epub 2015 Jan 6.

Abstract

A series of novel 1,2,3-triazole-pyrimidine-urea hybrids were designed, synthesized and evaluated for anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds 26, 30 and 38 exhibited excellent growth inhibition against B16-F10 with IC50 values of 32nM, 35nM and 42nM, respectively. Flow cytometry analysis demonstrated that compound 26 induced the cellular apoptosis in a concentration-dependent manner.

Keywords: Anticancer; Apoptosis; Pyrimidine; Triazole; Urea.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis
  • Triazoles / chemistry*
  • Triazoles / pharmacology
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis
  • Urea / pharmacology

Substances

  • Antineoplastic Agents
  • Pyrimidines
  • Triazoles
  • Urea
  • pyrimidine