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Current Pharmaceutical Design

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ISSN (Online): 1873-4286

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Review Article

2,5-Diketopiperazines (DKPs): Promising Scaffolds for Anticancer Agents

Author(s): Shaimaa S. Goher, Wessam S. Abdrabo, Giri Babu Veerakanellore and Bahaa Elgendy*

Volume 30, Issue 8, 2024

Published on: 09 February, 2024

Page: [597 - 623] Pages: 27

DOI: 10.2174/0113816128291798240201112916

Price: $65

Open Access Journals Promotions 2
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Abstract

2,5-Diketopiperazine (2,5-DKP) derivatives represent a family of secondary metabolites widely produced by bacteria, fungi, plants, animals, and marine organisms. Many natural products with DKP scaffolds exhibited various pharmacological activities such as antiviral, antifungal, antibacterial, and antitumor. 2,5-DKPs are recognized as privileged structures in medicinal chemistry, and compounds that incorporate the 2,5-DKP scaffold have been extensively investigated for their anticancer properties. This review is a thorough update on the anti-cancer activity of natural and synthesized 2,5-DKPs from 1997 to 2022. We have explored various aspects of 2,5-DKPs modifications and summarized their structure-activity relationships (SARs) to gain insight into their anticancer activities. We have also highlighted the novel approaches to enhance the specificity and pharmacokinetics of 2,5-DKP-based anticancer agents.

Keywords: 2, 5-Diketopiperazines (2, 5-DKPs), natural products, natural alkaloids, marine fungus, anticancer activities, pharmacological activities.

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