Amorfrutins are natural products characterized by isoprenoid-substituted benzoic acid derivatives. They are reported to be originally isolated from fruits of Amorpha fruticosa L. (bastard indigo) and from the roots of Glycyrrhiza foetida Desf. (licorice). Peroxisome proliferator-activated receptor gamma has emerged as a highly sought target for cancer and inflammatory diseases. Due to their promise in being partial agonist, and low µM activity, research efforts have been focused on developing structural derivatives with improved pharmacological properties, and low toxicity. We have devised a modular synthetic approach to generate a structurally diverse library of amorfrutin analogs. Since there have been no extensive studies done to evaluate the structure activity relationship (SAR), the first-generation analogs we have synthesized will shed light on the SAR of this class of natural products. We plan to evaluate the anti-cancer and anti-inflammatory principles in pertinent in vitro and in vivo models. The bioactivity data will guide us in designing the subsequent generations of analogs.

Chemical synthesis and biological evaluation of unnatural analogs of Amorfrutin

256th National Meeting (2018)

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