Biological applications of imiquimod analogues: An update (Review)

Obeid,Joelle; Shaito,Abdullah; El Hajj,Hiba; Deleuze‑masquefa,Carine; Bonnet,Pierre-Antoine; El‑Sabban,Marwan; Saliba,Jessica

doi:10.3892/wasj.2023.197

Biological applications of imiquimod analogues: An update (Review)

Authors:
- Joelle Obeid
- Abdullah Shaito
- Hiba El Hajj
- Carine Deleuze‑masquefa
- Pierre-Antoine Bonnet
- Marwan El‑Sabban
- Jessica Saliba
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Affiliations: Sorbonne University, INSERM, Nutrition and Obesity: Systemic Approaches, Nutriomics, 75006 Paris, France, Biomedical Research Center, Department of Biomedical Sciences at College of Health Sciences, and College of Medicine, Qatar University, Doha 2713, Qatar, Department of Experimental Pathology, Microbiology and Immunology, American University of Beirut, Beirut 1107, Lebanon, Institute of Biomolecules Max Mousseron (IBMM), UMR 5247, CNRS, ENSCM, Faculty of Pharmacy, Balard Chemistry Unit, Montpellier University, 34090 Montpellier, France, Institute of Biomolecules Max Mousseron (IBMM), UMR 5247, CNRS, ENSCM, Faculty of Pharmacy, Balard Chemistry Unit, Montpellier University, 34090 Montpellier, France, Department of Anatomy, Cell Biology and Physiological Sciences, Faculty of Medicine, American University of Beirut, Beirut 1107, Lebanon, Department of Biology, Faculty of Sciences, Lebanese University, Beirut 1533, Lebanon
Published online on: June 30, 2023 https://doi.org/10.3892/wasj.2023.197
Article Number: 20
Copyright : © Obeid et al. This is an open access article distributed under the terms of Creative Commons Attribution License [CC BY 4.0].

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Abstract

The last decade witnessed intensive efforts in drug discovery and the emergence of thousands of molecules with potential for use as therapeutic targets. However, only a few hundred of these molecules reached the stage of clinical trials, with only a handful being translated from the bench to bedside. One such example is imiquimod, an immune response modifier belonging to the imidazoquinoline family. Imiquimod was first approved by the US Food and Drug Administration for the topical treatment of anal and genital warts and actinic keratosis, and later exhibited a potent antitumor activity. This promising activity inspired the development of several imidazoquinoxaline analogues and derivatives. The present review provides a comprehensive overview of the scientific literature on the chemical synthesis of imiquimod and several of its analogues, namely EAPB0203, EAPB0503 and EABP02303. The present review also discusses their preclinical properties and mechanisms of action in the context of cancer and parasitic infections, highlighting the worthiness of translating these activities into therapeutic drugs.

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