Molecules (Aug 2022)

Synthesis, Anticancer Activities and Molecular Docking Studies of a Novel Class of 2-Phenyl-5,6,7,8-tetrahydroimidazo [1,2-<i>b</i>]pyridazine Derivatives Bearing Sulfonamides

  • Otmane Bourzikat,
  • Abdelmoula El Abbouchi,
  • Hamza Ghammaz,
  • Nabil El Brahmi,
  • Elmostfa El Fahime,
  • Arnaud Paris,
  • Richard Daniellou,
  • Franck Suzenet,
  • Gérald Guillaumet,
  • Saïd El Kazzouli

DOI
https://doi.org/10.3390/molecules27165238
Journal volume & issue
Vol. 27, no. 16
p. 5238

Abstract

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In the present study, new 2-phenyl-5,6,7,8-tetrahydroimidazo [1,2-b]pyridazines bearing sulfonamides were synthesized, characterized and evaluated for their anticancer activities. The structures of these derivatives were elucidated by 1H NMR, 13C NMR, infrared and high-resolution mass spectrometry for further validation of the target compound structures. The anticancer activities of the new molecules were evaluated against five human cancer cell lines, including A-549, Hs-683, MCF-7, SK-MEL-28 and B16-F10 cell lines using 5-fluorouracil and etoposide as the reference drugs. Among the tested compounds, 4e and 4f exhibited excellent activities in the same range of the positive controls, 5-fluorouracil and etoposide, against MCF-7 and SK-MEL-28 cancer cell lines, with IC50 values ranging from 1 to 10 μM. The molecular docking studies of 4e and 4f showed a strong binding with some kinases, which are linked to MCF-7 and SK-MEL-28 cancer cell lines.

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