| Popis: |
Natural products were once the only source of medicine and, since the dawn of modern drug discovery, have continued to serve as inspiration for the development of novel pharmaceuticals. The use of purified plant constituents greatly advanced the treatment of cancer towards the end of the 20th century. However, there remain many shortcomings with current treatment options with regards to toxicity, resistance, and overall effectiveness. The phyllanthusmin class of natural products, initially identified in 2006 to consist primarily of arylnaphthalene lignan arabinosyl glycosides, possess potent antiproliferative activity as well as a versatile pharmacophore whose exploration has recently been well studied, but not yet exploited into a known drug. The primary work described herein involves utilizing the phyllanthusmin scaffold to identify a novel anticancer lead compound, its mechanism of action, and develop novel synthetic routes in order to further streamline drug property optimization. |
