Confirmation of the Stereostructure of(+)-Cytostatin by Fluorous Mixture Synthesis of Four Candidate Stereoisomers

摘要

Cytostatin(1)is a potent and selective inhibitor of protein phosphatase 2A that was isolated from the cultured broth of Streptomyces sp.by Ishizuka and co-workers(Scheme 1).It inhibits lung metastasis of melanoma cells in mice and displays potent cytotoxic activity toward leukemia cell lines(inhibitory concentration;IC50=42-65 nM).Ishizuka and coworkers assigned the two-dimensional structure(constitution)of cytostatin(1)by analysis of 1D and 2D NMR spectra.