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

Area of Science:

• Medicinal Chemistry
• Natural Products Chemistry
• Pharmacology

Background:

• 2,5-Diketopiperazines (2,5-DKPs) are diverse secondary metabolites found across various organisms.
• DKP scaffolds are recognized as privileged structures with broad pharmacological activities, including anticancer properties.

Purpose of the Study:

• To provide a comprehensive review of anticancer activities of natural and synthesized 2,5-DKPs from 1997 to 2022.
• To explore modifications and summarize structure-activity relationships (SARs) of 2,5-DKPs for anticancer applications.
• To highlight novel approaches for enhancing the specificity and pharmacokinetics of 2,5-DKP-based anticancer agents.

Main Methods:

• Literature review of studies published between 1997 and 2022.
• Analysis of structural modifications and their impact on anticancer activity.
• Investigation of emerging strategies for drug development.

Main Results:

• Numerous natural and synthetic 2,5-DKPs exhibit potent anticancer activities.
• Structure-activity relationship studies provide insights into key molecular features for efficacy.
• Novel approaches show promise in improving drug targeting and pharmacokinetic profiles.

Conclusions:

• 2,5-DKPs represent a promising class of compounds for anticancer drug development.
• Understanding SARs is crucial for designing more effective and specific anticancer agents.
• Further research into novel delivery and modification strategies can optimize 2,5-DKP-based therapies.