title: Antineoplastic agents. 590. X-ray crystal structure of dolastatin 16 and syntheses of the dolamethylleuine and dolaphenvaline units.
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.
authors.affiliation: Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, PO Box 871604, Tempe, Arizona 85287-1604, United States. bpettit@asu.edu
authors.forename: George R
authors.initials: GR
authors.lastname: Pettit
authors.forename: Thomas H
authors.initials: TH
authors.lastname: Smith
authors.forename: Jun-Ping
authors.initials: JP
authors.lastname: Xu
authors.forename: Delbert L
authors.initials: DL
authors.lastname: Herald
authors.forename: Erik J
authors.initials: EJ
authors.lastname: Flahive
authors.forename: Collin R
authors.initials: CR
authors.lastname: Anderson
authors.forename: Paul E
authors.initials: PE
authors.lastname: Belcher
authors.forename: John C
authors.initials: JC
authors.lastname: Knight
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D047630:Depsipeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; C108201:dolastatin 16