Synthesis of some novel quinolines and pyrimido [4,5-b] quinolines bearing A sulfonamide moiety as potential anticancer and radioprotective agents

Arzneimittelforschung. 2007;57(12):795-803. doi: 10.1055/s-0031-1296682.

Abstract

Some novel 4-(quinolin-1-yl)-benzenesulfonamide and 4-(pyrimido[4,5-b]quinolin-10-yl)-benzenesulfonamide derivatives have been synthesized. All the newly synthesized target compounds were subjected to in vitro cytotoxic screening to be evaluated for their anticancer activity against Ehrlich ascites carcinoma cells. Among these new compounds, compounds 9a, 11, 12b, 18 and, in particular, 19 showed promising in vitro cytotoxic activity compared with doxorubicin (CAS 23214-92-8) as a reference drug. Moreover, compound 8 exhibited in vivo radioprotective activity against gamma-irradiation in mice.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Chemical Phenomena
  • Chemistry, Physical
  • Gamma Rays
  • Glutathione / blood
  • Humans
  • Indicators and Reagents
  • Lipid Peroxides / blood
  • Malondialdehyde / blood
  • Mice
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology*
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology*
  • Radiation-Protective Agents / chemical synthesis*
  • Radiation-Protective Agents / pharmacology*
  • Spectrophotometry, Infrared
  • Stereoisomerism
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology*
  • Superoxide Dismutase / blood

Substances

  • Antineoplastic Agents
  • Indicators and Reagents
  • Lipid Peroxides
  • Pyrimidinones
  • Quinolones
  • Radiation-Protective Agents
  • Sulfonamides
  • Malondialdehyde
  • Superoxide Dismutase
  • Glutathione