Abstract
A series of substituted chalcones was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. (E)-3-(3"-Hydroxy-4"-methoxyphenyl)-2-methyl-1-(3',4',5'- trimethoxyphenyl)-prop-2-en-1-one [IC50 (K562) 0.21 nM] was found to be the most active. A relationship between the conformation and cytotoxicity of the chalcones is discussed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / toxicity*
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Cell Cycle / drug effects
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Cell Division / drug effects
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Cell Survival / drug effects
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Chalcone / analogs & derivatives*
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Chalcone / chemical synthesis
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Chalcone / chemistry
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Chalcone / toxicity*
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Crystallography, X-Ray
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Drug Design
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Humans
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K562 Cells
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Models, Molecular
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Molecular Conformation
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Molecular Structure
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Chalcone