Synthesis of 2-oxo/thioxooctahydroquinazolin-5-one derivatives and their evaluation as anticancer agents

Chem Pharm Bull (Tokyo). 2010 Oct;58(10):1320-3. doi: 10.1248/cpb.58.1320.

Abstract

An environment friendly method for the synthesis of 2-oxo/thioxooctahydroquinazolin-5-one derivatives has been devised using Ceric ammonium nitrate (CAN) as catalyst and polyethylene glycol (PEG) as solvent. The cytotoxic effect of these compounds was studied on U87 human glioma cells, compounds 4c, 4d and 4e are found to exhibit excellent activity at a concentration as low as 0.06 µg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Agents / toxicity
  • Brain Neoplasms / drug therapy
  • Catalysis
  • Cell Line, Tumor
  • Cerium / chemistry
  • Humans
  • Polyethylene Glycols / chemistry
  • Quinazolinones / chemical synthesis
  • Quinazolinones / chemistry*
  • Quinazolinones / therapeutic use
  • Quinazolinones / toxicity

Substances

  • 4-(benzo(1,3)dioxol-5-yl)-2-thioxo-2,3,4,6,7,8-hexahydro-1H-quinazolin- 5-one
  • 4-ethyl-4,6,7,8-tetrahydro-1H,3H-quinazolin-2,5-dione
  • 4-propyl-4,6,7,8-tetrahydro-1H,3H-quinazolin-2,5-dione
  • Antineoplastic Agents
  • Quinazolinones
  • Cerium
  • Polyethylene Glycols
  • ceric ammonium nitrate