Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs |
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Authors: | Bryant Vashti C Kishore Kumar G D Nyong Abijah M Natarajan Amarnath |
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Affiliation: | Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, USA. |
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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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