Cargando…

Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Benassi, Alessandra, Doria, Filippo, Pirota, Valentina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7698752/
https://www.ncbi.nlm.nih.gov/pubmed/33217987
http://dx.doi.org/10.3390/ijms21228692
_version_ 1783615901619191808
author Benassi, Alessandra
Doria, Filippo
Pirota, Valentina
author_facet Benassi, Alessandra
Doria, Filippo
Pirota, Valentina
author_sort Benassi, Alessandra
collection PubMed
description 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.
format Online
Article
Text
id pubmed-7698752
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-76987522020-11-29 Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds Benassi, Alessandra Doria, Filippo Pirota, Valentina Int J Mol Sci Review 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. MDPI 2020-11-18 /pmc/articles/PMC7698752/ /pubmed/33217987 http://dx.doi.org/10.3390/ijms21228692 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Benassi, Alessandra
Doria, Filippo
Pirota, Valentina
Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title_full Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title_fullStr Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title_full_unstemmed Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title_short Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds
title_sort groundbreaking anticancer activity of highly diversified oxadiazole scaffolds
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7698752/
https://www.ncbi.nlm.nih.gov/pubmed/33217987
http://dx.doi.org/10.3390/ijms21228692
work_keys_str_mv AT benassialessandra groundbreakinganticanceractivityofhighlydiversifiedoxadiazolescaffolds
AT doriafilippo groundbreakinganticanceractivityofhighlydiversifiedoxadiazolescaffolds
AT pirotavalentina groundbreakinganticanceractivityofhighlydiversifiedoxadiazolescaffolds