Synthesis, characterization and in vitro anticancer evaluation of novel 1,2,4-triazolin-3-one derivatives

Eur J Med Chem. 2013 Apr:62:232-40. doi: 10.1016/j.ejmech.2013.01.004. Epub 2013 Jan 11.

Abstract

A series of novel 2-(4-chlorophenyl)-5-methyl-4-(2-amine/oxy-ethyl)-2,4-dihydro-[1,2,4]triazol-3-one (5a-t) were synthesized and in vitro anticancerous action of the resulting compounds was studied against NCI-60 Human Tumor Cell Line at a single high dose (10(-5) M) concentration for primary cytotoxicity assay. Among the tested compounds (5a-e, 5g-h, 5k, 5p), the compound 5g (NSC: 761736/1) was further evaluated for five dose criteria at five different minimal concentrations against the full panel of 60 human tumor cell lines which exhibited activity against Leukemia (GI50: 1.10 μM), Non-Small Cell Lung Cancer (GI50: 1.00 μM), Renal Cancer (GI50: 1.00 μM), Colon Cancer (GI50: 1.66 μM), CNS Cancer (GI50: 1.36 μM), Melanoma (GI50: 1.82 μM), Ovarian Cancer (GI50: 1.64 μM) and Breast Cancer (GI50: 1.69 μM).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Coumarins / chemical synthesis
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • 2-(4-chlorophenyl)-5-methyl-4-(2-(4-methyl-2-oxo-2H-chromen-7-yloxy)ethyl)-2H-1,2,4-triazol-3(4H)-one
  • Antineoplastic Agents
  • Coumarins
  • Triazoles