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Paper | Regular issue | Vol 104, No. 3, 2022, pp.447-469
Published online, 2nd December, 2021
DOI: 10.3987/COM-21-14578
Novel Pyrazolines and Benzothiazepines as Tubulin Polymerization Inhibitors: Synthesis, Biological Evaluation, and Molecular Docking

Alaadin E. Sarhan,* Ashraf A. Sediek, Nagy M. Khalifa, and Essam E. Hasan

*Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Institute, National Research Centre, Dokki, Cairo, 12622 Egypt


Synthesis, biological evaluation, and molecular docking of pyrazoline-linked benzenesulfonamides and diaryl 1,5-benzothiazepines prepared from new chalcones are described and elucidated. Novel compounds were studied for their in vitro anticancer profiles on HepG2, HEK-293, MCF-7, and MDA-MB-231 cancer cell lines, where, compounds IIb, III, and IVe demonstrated high to moderate cell proliferation inhibition activity. Compound IIb was further assessed for tubulin polymerization inhibition effects due to its high potency, which showed superior suppression compared to the reference drug. It induced cell cycle cessation at the G2/M phase and accumulation of cells in the pre-G1 phase, preventing its mitotic cycle. In addition, compound IIb activated caspase-7, mediating apoptosis of HepG2 cells. These findings, along with molecular docking and pharmacophore constructed models, provide a new scaffold of cytotoxic agents targeting tubulin.