Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates

Bioorg Med Chem Lett. 2016 Aug 15;26(16):3918-22. doi: 10.1016/j.bmcl.2016.07.012. Epub 2016 Jul 5.

Abstract

A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03μM and 2.46μM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase.

Keywords: Antiproliferative activity; Apoptosis; Chalcone; Dithiocarbamate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Apoptosis / drug effects
  • Caspase 3 / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chalcone / analogs & derivatives*
  • Chalcone / chemical synthesis
  • Chalcone / toxicity
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • G1 Phase Cell Cycle Checkpoints / drug effects
  • Humans
  • Structure-Activity Relationship
  • Thiocarbamates / chemical synthesis
  • Thiocarbamates / chemistry*
  • Thiocarbamates / toxicity
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • Antineoplastic Agents
  • Thiocarbamates
  • Tumor Suppressor Protein p53
  • Chalcone
  • Caspase 3