Glycyrrhetinic acid: a promising scaffold for the discovery of anticancer agents

Hidayat Hussain, Iftikhar Ali, Daijie Wang, Faruck L. Hakkim, Bernhard Westermann, Ishtiaq Ahmed, Ahmed M. Ashour, Amjad Khan, Amjad Hussain, Ivan R. Green, Syed Tasadaque Ali Shah

Research output: Contribution to journalReview articlepeer-review

26 Scopus citations


Introduction: Oleanane-type pentacyclic triterpenes named glycyrrhetinic acids (GAs) featuring a C-30 carboxylic acid group, are extracted from the licorice (Glycyrrhiza uralensis). Numerous biological properties of GA have been reported and have attracted researchers from all over the world in recent years due to the peculiar GA scaffold-based semisynthetic cytotoxic effects. Areas Covered: This review represents the applications of semisynthetic derivatives of GA for the development of future cancer treatments. Included in the review are important structural features of the semisynthetic GAs crucial for cytotoxic effects. Expert opinion: Numerous semisynthetic GA derivatives illustrated excellent cytotoxic effects toward various cancer cells. Notably the C-3(OH) at ring A along with C30-CO2H at ring E as vital structural features, make GA very appealing as a lead scaffold for medicinal chemistry, since these two groups permit the creation of further chemical diversity geared toward improved cytotoxic effects. Furthermore, numerous GA derivatives have been synthesized and indicate that compounds featuring cyanoenone moieties in ring A, or compounds having the amino group or nitrogen comprising heterocycles and hybrids thereof, illustrate more potent cytotoxicity. Furthermore, GA has a great capability to be conjugated with other anticancer molecules to synergistically enhance their combined cytotoxicity.

Original languageEnglish (US)
Pages (from-to)1497-1516
Number of pages20
JournalExpert Opinion on Drug Discovery
Issue number12
StatePublished - 2021

Bibliographical note

Funding Information:
This manuscript has not been funded.

Publisher Copyright:
© 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.


  • Glycyrrhetinic acid
  • cytotoxicity
  • derivatives
  • lead compounds
  • licorice
  • mode of action


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