Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds.

International Journal of Molecular Sciences
Alessandra BenassiValentina Pirota

Abstract

Nowadays, an increasing number of heterocyclic-based drugs found application in medicinal chemistry and, in particular, as anticancer agents. In this context, oxadiazoles-five-membered aromatic rings-emerged for their interesting biological properties. Modification of oxadiazole scaffolds represents a valid strategy to increase their anticancer activity, especially on 1,2,4 and 1,3,4 regioisomers. In the last years, an increasing number of oxadiazole derivatives, with remarkable cytotoxicity for several tumor lines, were identified. Structural modifications, that ensure higher cytotoxicity towards malignant cells, represent a solid starting point in the development of novel oxadiazole-based drugs. To increase the specificity of this strategy, outstanding oxadiazole scaffolds have been designed to selectively interact with biological targets, including enzymes, globular proteins, and nucleic acids, showing more promising antitumor effects. In the present work, we aim to provide a comprehensive overview of the anticancer activity of these heterocycles, describing their effect on different targets and highlighting how their structural versatility has been exploited to modulate their biological properties.

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Citations

Mar 7, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Bimal Krishna BanikPreetismita Borah
May 1, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lamya H Al-WahaibiAli A El-Emam
May 1, 2021·International Journal of Molecular Sciences·Antonio Palumbo Piccionello
Jun 3, 2021·Pharmaceuticals·Camelia Elena StecozaMirela Mihaila
Sep 14, 2021·Journal of Agricultural and Food Chemistry·Feng PengWei Xue

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Methods Mentioned

BETA
acetylation
xenograft
xenografts
flow cytometry
dot blot
circular dichroism
FRET
fluorescence microscopy

Clinical Trials Mentioned

NCT00554229
NCT02260661

Software Mentioned

Discovery Studio
AutoDock

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