Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Version 1 : Received: 30 October 2020 / Approved: 2 November 2020 / Online: 2 November 2020 (11:18:22 CET)

A peer-reviewed article of this Preprint also exists.

Benassi, A.; Doria, F.; Pirota, V. Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds. Int. J. Mol. Sci. 2020, 21, 8692. Benassi, A.; Doria, F.; Pirota, V. Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds. Int. J. Mol. Sci. 2020, 21, 8692.

Journal reference: Int. J. Mol. Sci. 2020, 21, 8692
DOI: 10.3390/ijms21228692

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 oxadiazoles-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.

Subject Areas

Oxadiazoles; Bioactive heterocyclics; anticancer agents; Telomerase; Carbonic anhydrase; Histone deacetylase; Kinases; Tubulin; DNA; G-quadruplex.

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