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Bioorg Med Chem. 2001 Jan;9(1):57-67.

Participation of the beta-hydroxyketone part for potent cytotoxicity of callystatin A, a spongean polyketide.

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  • 1Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Japan.


The participation of the beta-hydroxyketone part of callystatin A in the potent cytotoxicity was analyzed through the analogue-syntheses and the assessment of their biological potencies. The ketonic carbonyl, the 19-hydroxyl, and the three asymmetric methyl groups located in the beta-hydroxyketone part of callystatin A were revealed to contribute to the cytotoxic potency, respectively. Moreover, the alpha,beta-unsaturated delta-lactone portion was shown to serve as a conclusive functional group for the cytotoxic activity.

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