Title:Oxadiazole Derivatives as Anticancer and Immunomodulatory
Agents: A Systematic Review
Volume: 30
Issue: 30
Author(s): Héverton Mendes Araújo, Gabriel Acácio de Moura, Yasmim Mendes Rocha, João Pedro Viana Rodrigues and Roberto Nicolete*
Affiliation:
- Department of Pharmacy, Federal University of Ceará (UFC), Fortaleza - CE, Brazil and Oswaldo Cruz
Foundation (Fiocruz Ceará), Eusébio - CE, Brazil
Keywords:
Oxadiazoles, cancer, immunomodulation, inflammatory mediators, macrophages, chemotherapy.
Abstract:
Background: Tumor plasticity processes impact the treatment of different
types of cancer; as an effect of this, the bioprospecting of therapies from natural and/or
synthetic compounds that can regulate or modulate the immune system has increased considerably.
Oxadiazole derivatives are structures that exhibit diverse biological activities.
Therefore, this review aimed to evaluate the activity of oxadiazole compounds against tumor
cell lines and their possible immune-mediated mechanisms.
Methods: A search in PubMed, Web of Science, and Science Direct databases was carried
out on studies published from January 1, 2004, to January 31, 2022, using “oxadiazole”
in combination with the other descriptors “cancer” and “macrophage”. Only experimental
in vitro and in vivo articles were included. A similar search strategy was used in
the Derwent Innovation Index database for technology mapping. The search was performed
on Drugbank using the descriptor oxadiazole for commercial mapping.
Results: 23 oxadiazole studies were included in this review, and some biological activities
linked to antitumoral and immunomodulation were listed. Oxadiazole derivatives inhibited
tumor cell growth and proliferation, blocked cell cycle, modulated mitochondrial
membrane potential, presented immunoregulatory activity by different mechanisms reducing
proinflammatory cytokines levels and acted directly as selective inhibitors of the
COX enzyme. There was an increase in oxadiazole patent publications in the last 11
years, with emphasis on chemistry, pharmacy and biotechnology applied to microbiology
areas. Compounds with 1,2,4-oxadiazole isomer are predominant in patent publications
and approved drugs as observed in the technological and commercial mapping.
Conclusion: Therefore, oxadiazole derivatives are therapeutic molecules that can be considered
promising for the development of cancer therapies.