Antineoplastic Agents. 590. X-ray Crystal Structure of Dolastatin 16 and Syntheses of the Dolamethylleuine and Dolaphenvaline Units
Journal of Natural Products2011Vol. 74(5), pp. 1003–1008
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George R. Pettit, Thomas H. Smith, Jun‐Ping Xu, Delbert L. Herald, Erik J. Flahive, Collin R. Anderson, Paul E. Belcher, John Knight
Abstract
Three advances necessary to bring dolastatin 16 (1) into full-scale preclinical development as an anticancer drug have been accomplished. The X-ray crystal structure of dolastatin 16 has been solved, which allowed stereoselective syntheses of its two new amino acid units, dolamethylleuine (Dml) and dolaphenvaline (Dpv), to be completed. The X-ray crystal structures of synthetic Z-Dml and TFA-Dpv have also been completed.
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