Synthesis, in-vitro anticancer screening and radiosensitizing evaluation of some new N-(quinoxalin-2-yl)benzenesulfonamide derivatives

Arzneimittelforschung. 2012 Jan;62(1):46-52. doi: 10.1055/s-0031-1295496. Epub 2012 Jan 10.

Abstract

The objective of this work is to synthesize and investigate the anticancer activity of a new series of sulfaquinoxaline derivatives by incorporating biologically active moieties (thiourethane, thiazole, imidazole, imidazopyrimidine, imidazopyrimido-pyrimidine, thienopyrimidine, benzopyrimidinone, benzothiazole, thiazole and pyridine moieties). All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human liver cell line (HEPG2). All the tested compounds showed comparable activity to that of the reference drug 5-fluorouracil (IC50=40 µM), and the most potent compounds were found to be compounds 4 and 17 (IC50=4.29 and 11.27 µM, respectively). On the other hand, the most potent compounds 4 and 17 were evaluated as radiosensitizing agents.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Benzenesulfonamides
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Radiation-Sensitizing Agents / chemical synthesis*
  • Radiation-Sensitizing Agents / pharmacology
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology

Substances

  • Antineoplastic Agents
  • Radiation-Sensitizing Agents
  • Sulfonamides