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

一类新型含磺胺类2-苯基-5,6,7,8-四氢咪唑并[1,2-b]哒嗪衍生物的合成、抗癌活性及分子对接研究

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

Abstract

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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