Abstract
Recently a series of arylnaphthalene lignans was isolated from Phyllanthus poilanei by the Kinghorn lab. These compounds bear a strong structural resemblance to etoposide, a semi-synthetic DNA topoisomerase II (topo II) poison, and the natural product podophyllotoxin. Although the newly isolated compounds do not appear to act on topo II, they have demonstrated potent in vitro antiproliferative activity against HT-29 human colon cancer cells. Moreover, one of these compounds, phyllanthusmin D, also showed promising activity in a hollow fiber assay using HT-29 cells in mice. In an effort to understand the basic structure-activity requirements of this class of natural product and to remedy the limited aqueous solubility of these molecules, a series of structural analogues were synthesized and tested for biological activity. These studies have focused primarily on the role of the saccharide moiety in the activity of this class, although variation of the aryl substituents has also been examined.
Published Version
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