Antineoplastic Agents. 590. X-ray Crystal Structure of Dolastatin 16 and Syntheses of the Dolamethylleuine and Dolaphenvaline Units

作者:Pettit George R*; Smith Thomas H; Xu Jun Ping; Herald Delbert L; Flahive Erik J; Anderson Collin R; Belcher Paul E; Knight John C
来源:Journal of Natural Products, 2011, 74(5): 1003-1008.
DOI:10.1021/np100877h

摘要

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.

  • 出版日期2011-5