Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

• Published in: Molecules (Basel, Switzerland) Vol. 25; no. 15; p. 3457
• Main Authors: Brullo, Chiara, Rapetti, Federica, Bruno, Olga
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI 29.07.2020; MDPI AG
• Subjects: anti-inflammatory agents; anti-pathogens agents; anticancer agents; Chemistry Techniques, Synthetic; Chemistry, Pharmaceutical - methods; Humans; Pharmaceutical Preparations - chemical synthesis; Pharmaceutical Preparations - chemistry; protein kinase inhibitors; pyrazole nucleus; Pyrazoles - chemistry; pyrazolyl-ureas; Review; Structure-Activity Relationship; Urea - chemistry; pyrazolyl-ureas; anti-inflammatory agents; anti-pathogens agents; pyrazole nucleus; protein kinase inhibitors; anticancer agents
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules25153457

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.