Pharmacophore optimization of imidazole chalcones to modulate microtubule dynamics

Bioorganic Chemistry(2022)

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摘要
•Structure-activity relationship of imidazole chalcone mimics.•Cytotoxic with IC50 values in the upper nanomolar to low micromolar range.•Compounds caused mitotic arrest of HeLa cells.•Compounds induced dramatic disassembly of the mitotic spindle.•Docking studies show binding to colchicine binding site.
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关键词
Antimitotic agents,SAR,Imidazole chalcones,Mitotic spindle,Microtubule dynamics
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