The synthesis and antiproliferative activities of new arylidene-hydrazinyl-thiazole derivatives

Int J Mol Sci. 2014 Dec 1;15(12):22059-72. doi: 10.3390/ijms151222059.

Abstract

New and known arylidene-hydrazinyl-thiazole derivatives have been synthesized by a convenient Hantzsch condensation. All compounds were evaluated for their in vitro cytotoxicity on two carcinoma cell lines, MDA-MB231 and HeLa. Significant antiproliferative activity for 2-(2-benzyliden-hydrazinyl)-4-methylthiazole on both MDA-MB-231 (IC50: 3.92 µg/mL) and HeLa (IC50: 11.4 µg/mL) cell lines, and for 2-[2-(4-methoxybenzylidene) hydrazinyl]-4-phenylthiazole on HeLa (IC50: 11.1 µg/mL) cell line is reported. Electrophoresis experiments showed no plasmid DNA (pTZ57R) cleavage in the presence of the investigated thiazoles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death / drug effects
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • DNA / metabolism
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Humans
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • Inhibitory Concentration 50
  • Intercalating Agents / pharmacology
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*

Substances

  • Hydrazines
  • Intercalating Agents
  • Thiazoles
  • DNA