Cargando…

Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

The pyrazole nucleus has long been known as a privileged scaffold in the synthesis of biologically active compounds. Within the numerous pyrazole derivatives developed as potential drugs, this review is focused on molecules characterized by a urea function directly linked to the pyrazole nucleus in...

Descripción completa

Detalles Bibliográficos
Autores principales: Brullo, Chiara, Rapetti, Federica, Bruno, Olga
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7435939/
https://www.ncbi.nlm.nih.gov/pubmed/32751358
http://dx.doi.org/10.3390/molecules25153457
_version_ 1783572438944055296
author Brullo, Chiara
Rapetti, Federica
Bruno, Olga
author_facet Brullo, Chiara
Rapetti, Federica
Bruno, Olga
author_sort Brullo, Chiara
collection PubMed
description The pyrazole nucleus has long been known as a privileged scaffold in the synthesis of biologically active compounds. Within the numerous pyrazole derivatives developed as potential drugs, this review is focused on molecules characterized by a urea function directly linked to the pyrazole nucleus in a different position. In the last 20 years, the interest of numerous researchers has been especially attracted by pyrazolyl-ureas showing a wide spectrum of biological activities, ranging from the antipathogenic activities (bacteria, plasmodium, toxoplasma, and others) to the anticarcinogenic activities. In particular, in the anticancer field, pyrazolyl-ureas have been shown to interact at the intracellular level on many pathways, in particular on different kinases such as Src, p38-MAPK, TrKa, and others. In addition, some of them evidenced an antiangiogenic potential that deserves to be explored. This review therefore summarizes all these biological data (from 2000 to date), including patented compounds.
format Online
Article
Text
id pubmed-7435939
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-74359392020-08-24 Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry Brullo, Chiara Rapetti, Federica Bruno, Olga Molecules Review The pyrazole nucleus has long been known as a privileged scaffold in the synthesis of biologically active compounds. Within the numerous pyrazole derivatives developed as potential drugs, this review is focused on molecules characterized by a urea function directly linked to the pyrazole nucleus in a different position. In the last 20 years, the interest of numerous researchers has been especially attracted by pyrazolyl-ureas showing a wide spectrum of biological activities, ranging from the antipathogenic activities (bacteria, plasmodium, toxoplasma, and others) to the anticarcinogenic activities. In particular, in the anticancer field, pyrazolyl-ureas have been shown to interact at the intracellular level on many pathways, in particular on different kinases such as Src, p38-MAPK, TrKa, and others. In addition, some of them evidenced an antiangiogenic potential that deserves to be explored. This review therefore summarizes all these biological data (from 2000 to date), including patented compounds. MDPI 2020-07-29 /pmc/articles/PMC7435939/ /pubmed/32751358 http://dx.doi.org/10.3390/molecules25153457 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
Brullo, Chiara
Rapetti, Federica
Bruno, Olga
Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title_full Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title_fullStr Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title_full_unstemmed Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title_short Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
title_sort pyrazolyl-ureas as interesting scaffold in medicinal chemistry
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7435939/
https://www.ncbi.nlm.nih.gov/pubmed/32751358
http://dx.doi.org/10.3390/molecules25153457
work_keys_str_mv AT brullochiara pyrazolylureasasinterestingscaffoldinmedicinalchemistry
AT rapettifederica pyrazolylureasasinterestingscaffoldinmedicinalchemistry
AT brunoolga pyrazolylureasasinterestingscaffoldinmedicinalchemistry