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Open Access Publications from the University of California

Design, synthesis and in vitro splicing inhibition of desmethyl and carba-derivatives of herboxidiene.

  • Author(s): Ghosh, Arun K
  • Lv, Kai
  • Ma, Nianchun
  • Cárdenas, Emilio L
  • Effenberger, Kerstin A
  • Jurica, Melissa S
  • et al.

Herboxidiene is a potent inhibitor of spliceosomes. It exhibits excellent anticancer activity against multiple human cancer cell lines. Herein, we describe an enantioselective synthesis of a desmethyl derivative and the corresponding carba-derivatives of herboxidiene. The synthesis involved Suzuki coupling of a vinyl iodide with boronate as the key reaction. For the synthesis of carba-derivatives, the corresponding optically active cyclohexane-1,3-dicarbonyl derivatives were synthesized using an enantioselective desymmetrization of meso-anhydride. The biological properties of these derivatives were evaluated in an in vitro splicing assay.

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