Abstract
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.
Recent Patents on Anti-Cancer Drug Discovery
Title:Journey Describing the Cytotoxic Potential of Withanolides: A Patent Review
Volume: 13 Issue: 4
Author(s): Hidayat Hussain*, Rene Csuk, Ivan R. Green, Najeeb Ur Rehman, Ghulam Abbas and Wahid Hussain
Affiliation:
- Leibniz Institute of Plant Biochemistry, Department of Bioorganic Chemistry, Weinberg 3, D-06120 Halle (Salle),Germany
Keywords: Anticancer, drug discovery, ergostane steroids, in vitro, natural products, withanolide.
Abstract: 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.
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Hussain Hidayat *, Csuk Rene , Green R. Ivan , Ur Rehman Najeeb , Abbas Ghulam and Hussain Wahid , Journey Describing the Cytotoxic Potential of Withanolides: A Patent Review, Recent Patents on Anti-Cancer Drug Discovery 2018; 13 (4) . https://dx.doi.org/10.2174/1574892813666180808154928
DOI https://dx.doi.org/10.2174/1574892813666180808154928 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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