title: Radiosynthesis of antitumor spliceosome modulators.
abstract: A set of novel antitumor agents (the sudemycins) has recently been described that are analogs of the natural product FR901464. We report the radiosynthesis of two of these antitumor drug lead compounds, using a three step procedure: (1) ester hydrolysis, (2) Lindlar's catalyst/tritium gas to give a (S,Z)-4-acetoxypent-2-enoic acid derivative, and finally (3) amide bond formation. These labeled analogs are useful in developing a better understanding of the pharmacological properties of this new class of therapeutic lead compounds.
authors.affiliation: Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.
authors.forename: Tinopiwa
authors.initials: T
authors.lastname: Goronga
authors.forename: Vincent A
authors.initials: VA
authors.lastname: Boyd
authors.forename: Chandraiah
authors.initials: C
authors.lastname: Lagisetti
authors.forename: Cynthia
authors.initials: C
authors.lastname: Jeffries
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Webb
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D007553:Isotope Labeling / Q000379:methods*; D011714:Pyrans / Q000737:chemistry; D013141:Spiro Compounds / Q000737:chemistry; D017381:Spliceosomes / Q000187:drug effects; D014316:Tritium
chemical_list: D000970:Antineoplastic Agents; C104486:FR 901464; D011714:Pyrans; D013141:Spiro Compounds; D014316:Tritium