Withanolides are C-28 ergostane steroids known to demonstrate some very interesting
therapeutic properties. Numerous withanolides have been isolated from a variety of different plant species
and can be employed to treat various types of cancers. Withanolides are indeed capable of demonstrating
excellent anticancer, anti-inflammatory, and neuroprotective activities. Additionally, libraries
of prepared withaferin A analogs incorporating an acyl, sulphate, amide and aldehyde functionality
have demonstrated the most potential response. It is of particular interest to note that an acetyl group at
either C-4, C-19 or C-27 enhances the anticancer effects. Since the majority of natural withanolides
reported in patents are classified as “Type-A”, it is our opinion that there should now be a focus on
developing “Type-B” withanolides and an investigation into their various therapeutic applications.
Moreover, very little real innovation in synthetic methodologies has been reported which opens up
huge possibilities for novel synthetic methodologies to be developed for the production of larger libraries
new withanolides and their analogs to incorporate chemical diversity. In addition, since withanolides
have the capability to conjugate with other anticancer compounds, this should encourage scientists
to prepare lead compounds in cancer drug discovery.
Keywords: Anticancer, drug discovery, ergostane steroids, in vitro, natural products, withanolide.
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