A Review: Exploring Synthetic Schemes and Structure-activity Relationship (SAR) Studies of Mono-carbonyl Curcumin Analogues for Cytotoxicity Inhibitory Anticancer Activity

Curr Org Synth. 2023;20(8):821-837. doi: 10.2174/1570179420666230126142238.

Abstract

Introduction: Cancer is the major cause of death globally. Cancer can be treated with naturally occurring Curcumin nuclei. Curcumin has a wide range of biological actions, including anti-inflammatory and anti-cancer properties. Even though it is an effective medicinal entity, it has some limitations such as instability at physiological pH and a weak pharmacokinetic profile due to the β-diketone moiety present in it. To overcome this drawback, research was carried out on monoketone moieties in curcumin, popularly known as mono-carbonyl curcumin.

Objective: The present review focuses on different synthetic schemes and Mono-carbonyl curcumin derivative's Structure-Activity Relationship (SAR) as a cytotoxic inhibitory anticancer agent. The various synthetic schemes published by researchers were compiled.

Methods: Findings of different researchers working on mono-carbonyl curcumin as an anticancer have been reviewed, analyzed and the outcomes were summarized.

Results: The combination of all of these approaches serves as a one-stop solution for mono-carbonyl curcumin synthesis. The important groups on different positions of mono-carbonyl curcumin were discovered by a SAR study focused on cytotoxicity, which could be useful in the designing of its derivatives.

Conclusion: Based on our examination of the literature, we believe that this review will help researchers design and develop powerful mono-carbonyl curcumin derivatives that can be proven essential for anticancer activity.

Keywords: Mono-carbonyl curcumin; anticancer activity; cytotoxicity; pharmacokinetic profile; structure-activity relationship; synthetic schemes.

Publication types

  • Review

MeSH terms

  • Anti-Inflammatory Agents / pharmacology
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Curcumin* / chemistry
  • Curcumin* / pharmacology
  • Ketones / chemistry
  • Structure-Activity Relationship

Substances

  • Curcumin
  • Antineoplastic Agents
  • Anti-Inflammatory Agents
  • Ketones