Natural products have proven to be useful lead compounds in part due to their densely functionalized cores and abundant chirality. For example, arylnaphthalene lignan lactone containing natural products have been recognized as an important class of compounds due to their cytotoxicity against an array of different human cancer cell lines and, therefore, have been the focus of a number of drug development studies. The phyllanthusmins represent a specific subclass of arylnaphthalene lignan lactones isolated from the plant <i>Phyllanthus poilanei</i>. These natural products and structurally related synthetic analogues show moderate to good antiproliferative activity against ovarian cancer cell lines and have previously displayed anticancer activity in colon cancer cell lines. Preliminary structure-activity relationship studies on this class of compounds focused on functionalization of the diphyllin portion of the phyllanthusmins. Our current research, however, has focused on selective functionalization of the gylcone portion of the compound, specifically through further development of the galactose moiety of PHY-34, an analogue that has shown potent in vivo efficacy in an OVCAR-8 xenograft model.

Glycone manipulation as a general strategy of optimizing the drug properties of the phyllanthusmin class of natural products

2019 Fall National Meeting

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