UC Santa Cruz
Enantioselective synthesis of spliceostatin e and evaluation of biological activity
- Author(s): Ghosh, AK
- Veitschegger, AM
- Sheri, VR
- Effenberger, KA
- Prichard, BE
- Jurica, MS
- et al.
Published Web Locationhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC4260646/
© 2014 American Chemical Society. An enantioselective total synthesis of spliceostatin E has been accomplished. The δ-lactone unit A was constructed from readily available (R)-glycidyl alcohol using a ring-closing olefin metathesis as the key reaction. A cross-metathesis of ring A containing δ-lactone and the functionalized tetrahydropyran B-ring provided spliceostatin E. Our biological evaluation of synthetic spliceostatin E revealed that it does not inhibit splicing in vitro and does not impact speckle morphology in cells. Spliceostatin E was reported to possess potent antitumor activity.
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