The Role of Substituents of ar-Turmerone for its Anticancer Activity

For the evaluation of the role of substituents of ar-turmerone for its anticancer activity, ar-turmerone (1a) and its analogs like 2-methyl-6-(4'-methyphenyl)-2-octen-4-one (1b), 2-methyl-6-phenyl-2-hepten-4-one (1c), 2-methyl-6-phenyl-2-octen-4-one (1d) and 2 methyl-6-(trans-4'-methylcyclohexyl)-2-hepten-4-one (1e) were preparedd and their cytotoxic activities against $L_{1210}$ cell were determined. Omission of methyl group at para-position dose not variate the cytotoxicity of ar-turmerone. Elongation of alkyl group at 6-position decreases $ED_{50}$ value. Saturation of aromatic ring of ar-turmerone markedly decreases the cytotoxicity. Therefore the smaller size of alkyl group at 6-position and aromatic ring of ar-turmerone should be essential for exhibiting its anticancer activity.