Synthesis, anticancer and radiosensitizing evaluation of some novel sulfonamide derivatives

•Novel sulfonamide derivatives were synthesized.•Novel sulfonamide chalcones were synthesized.•In-vitro anticancer evaluation on HEPG2 cell line.•Radiosensitizing evaluation for the most potent compounds.

In this study, novel series of sulfonamide derivatives were synthesized starting from 2-cyanoacetyl)hydrazono)ethyl)phenyl)benzenesulfonamide 4a and 2-cyanoacetyl)hydrazono)ethyl)phenyl)-4-methylbenzenesulfonamide 4b. Different biologically active moieties as pyrazol, thiophene, pyridine and pyrimidines were introduced in order to investigate their in-vitro anticancer activity, in addition to a novel series of sulfonamide chalcones were synthesized from the reported 4-acetyl-N-(P-tolyl) benzenesulfonamide 3b. The newly synthesized sulfonamide derivatives were characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses and were tested for their in-vitro anticancer activity against human tumor liver cell line (HEPG-2). The most potent compounds in this study were compounds 4a, 4b, 5a, 6a, 6b, 8, 9, 11, 13, 18 and 19 which showed higher activity than doxorubicin with IC50 ranging from 11.0 to 31.8 μM. Additionally, eight compounds among the most potent were evaluated for their ability to enhance the cell killing effect of γ-radiation.

Graphical abstractNovel series of sulfonamide derivatives were synthesized. The most potent compounds in this study were compounds 4a, 4b, 5a, 6a, 6b, 8, 9, 12, 13, 18 and 19. Eight compounds among the most potent were evaluated for their radiosensitizing activity.Figure optionsDownload full-size imageDownload as PowerPoint slide