Heterocycles in Breast Cancer Treatment: The Use of Pyrazole Derivatives

Abstract

Among the aromatic heterocycle rings, pyrazole –a five-membered ring with two adjacent nitrogen atoms in its structure– has been postulated as a potent candidate in the pharmacological context. This moiety is an interesting therapeutic target covering a broad spectrum of biological activities due to its presence in many natural substances. Hence, the potential of the pyrazole derivatives as antitumor agents has been explored in many investigations, showing promising results in some cases. In this sense, breast cancer, which is already the leading cause of cancer mortality in women in some countries, has been the topic selected for this review, which covers a range of different research from the earliest studies published in 2003 to the most recent ones in 2021.

Synthesis, In Vitro Biological Investigation, and In Silico Analysis of Pyrazole-Based Derivatives as Multi-target Agents

“…The diseases-related complications and causes Pyrazole (five-membered ring with two nitrogen atoms) is a pharmacophore moiety. Pyrazole-based derivatives exhibit various biological activities [8][9][10]. Pyrazole-based Schiff base I possessed significant in vitro cytotoxic properties against HeLa Egyptian Journal of Chemistry http://ejchem.journals.ekb.eg/ ________________________________________________ Egypt.…”

Recent advances in anticancer drug discovery: A review

“…57 Due to its presence in many natural substances, pyrazole, a five-membered ring with two adjacent nitrogen atoms in its structure, has been postulated as a potent candidate in the pharmacological context with an interesting therapeutic target covering a broad spectrum of biological activities. 58 In vitro tests recently revealed progress in the use of bisheterocyclic compounds as efficient anticancer treatments, which goes beyond the concern regarding the anticancer treatment potential of heterocyclic compounds. 59…”

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].…”