Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

Abstract

Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical structures that confer them with a broad spectrum of pharmacological activities. They have been extensively explored for designing potent and selective anticancer agents. In recent years, numerous pyrazole derivatives have been synthesized and evaluated for their anticancer potential against various cancer cell lines. Structure–activity relationship studies have shown that appropriate substitution on different positions of the pyrazole ring can significantly enhance anticancer efficacy and tumor selectivity. It is noteworthy that many pyrazole derivatives have demonstrated multiple mechanisms of anticancer action by interacting with various targets including tubulin, EGFR, CDK, BTK, and DNA. Therefore, this review summarizes the current understanding on the structural features of pyrazole derivatives and their structure-activity relationships with different targets, aiming to facilitate the development of potential pyrazole-based anticancer drugs. We focus on the latest research advances in anticancer activities of pyrazole compounds reported from 2018 to present.

Structure–Activity Relationship Studies on Highly Functionalized Pyrazole Hydrazones and Amides as Antiproliferative and Antioxidant Agents

“…Pyrazole scaffold is a pharmaceutically relevant moiety [1][2][3][4][5][6], and pyrazole-containing compounds show antiviral [7], antibacterial [8,9], antimalarial [10], anti-inflammatory [11], antidiabetic [12], antiglaucoma [13,14], and anticancer [15][16][17][18][19][20][21] properties. Furthermore, pyrazole scaffolds are shared by several protein kinase inhibitors, including FDA-approved drugs Avapritinib, Asciminib, Crizotinib, Encorafenib, Erdafitinib, Pralsetinib, Pirtobrutinib, and Ruxolitinib (Figure 1) [22,23].…”

Evaluation of Antitumor Activity of Xanthones Conjugated with Amino Acids

“…The use of scaffolds for drug discovery allows for the exploration of different chemicals, providing structural templates to optimize molecules with potential anticancer activity. For example, heterocyclic building blocks, like thiophenes, pirrole, or pyrazoles, demonstrated high efficiency in the treatment of different types of cancer, including metastatic models [3][4][5][6]. Over eighty-five percent of FDA-approved molecules contain heterocycles and have indicated potential benefits against a range of cancer treatments [7].…”

A Proteomics Approach Identifies RREB1 as a Crucial Molecular Target of Imidazo–Pyrazole Treatment in SKMEL-28 Melanoma Cells

“…This versatility allows the pyrazole ring to be incorporated into a vast number of chemical compounds [ 2 ]. Nowadays, due to their pharmacological properties, pyrazole derivatives are broadly employed as drugs in the treatment of inflammation, pain, infections, obesity, cancer, and so forth [ 3 , 4 ].…”