2. Academic Validation
  3. Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs

Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):245-8. doi: 10.1016/j.bmcl.2011.11.025.
Vashti C Bryant 1,  G D Kishore Kumar,  Abijah M Nyong,  Amarnath Natarajan
Affiliations

Affiliation

  • 1 Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, USA.
PMID: 22137846 DOI: 10.1016/j.bmcl.2011.11.025
Abstract

The macrocyclic diarylether heptanoid (MDEH) Natural Products have been used in folk medicine for centuries. MDEHs are reported to exert anti-tumor properties by inhibiting the activation of NF-κB. Here we report the synthesis of a small MDEH library (first reported synthesis of racemic platycarynol) using a Grubbs cross metathesis/Ullmann cyclization strategy. Evaluation of the library led to the identification of MDEH 9b which sensitizes pancreatic Cancer cells to gemcitabine mediated growth inhibition and Apoptosis.

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