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A series of 3-methylidenetetrahydro-2-furanones 7 bearing various hydroxyalkyl substituents in position 5 were synthesized using novel diastereo- and enantioselective methodology. In vitro cytotoxicity data demonstrated that all prepared compounds were active against L-1210 and HL-60 tissue culture cells with 7e being the most potent (IC(50) = 6.9 microM). Also an increase in activity with an increase in lipophilicity of the substituents in the order H < alkyl < phenyl was observed.
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Janecki et al. (2002) studied this question.
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