Synthesis, in-vitro Anticancer Screening and Radiosensitizing Evaluation of some New N-(quinoxalin-2-yl)benzenesulfonamide Derivatives

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.

Key words

sulfonamide - quinoxaline - anticancer - radiosensitizing

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