Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011–2020): Current Status and Future Prospects

Abstract

Pyrazole has been recognized as a pharmacologically important privileged scaffold whose derivatives produce almost all types of pharmacological activities and have attracted much attention in the last decades. Of the various pyrazole derivatives reported as potential therapeutic agents, this article focuses on pyrazole-based kinase inhibitors. Pyrazole-possessing kinase inhibitors play a crucial role in various disease areas, especially in many cancer types such as lymphoma, breast cancer, melanoma, cervical cancer, and others in addition to inflammation and neurodegenerative disorders. In this article, we reviewed the structural and biological characteristics of the pyrazole derivatives recently reported as kinase inhibitors and classified them according to their target kinases in a chronological order. We reviewed the reports including pyrazole derivatives as kinase inhibitors published during the past decade (2011–2020).

Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents

“…There are many reviews that present and demonstrate the anticancer potential of the pyrazole ring, unfused or fused in structures like indazole or pyrazolopyrimidines, but these works present only on the active derivatives [ 32 , 33 , 34 , 35 , 36 , 37 , 38 ]. The researchers tend to publish only works with positive results in order to maximize their scientific impact.…”

Fluorinated and Non-Fluorinated 1,4-Diarylpyrazoles via MnO2-Mediated Mechanochemical Deacylative Oxidation of 5-Acylpyrazolines

“…Due to the discovery of a number of practical applications, there is increasing interest in the chemistry of pyrazole-based compounds, and fluorinated analogues are of special significance in medicine, crop protection, as well as material sciences [ 1 , 2 , 3 , 4 ]. The title heterocycle constitutes a key structural element of pharmaceuticals and agrochemicals; they exhibit a variety of biological activities such as being anti-inflammatory (e.g., Celecoxib, Lonazolac), antibacterial, anticancer (e.g., Crizotinib), anti-obesity (e.g., Rimonabant), antidepressant (e.g., Fezolamine), antiviral (e.g., Lenacapavir), and antifungal (e.g., Penthiopyrad), and have been widely applied as pesticides ( Figure 1 ) [ 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 , 13 ]. In addition, some pyrazoles have been successfully applied in polymer chemistry, as well as for the preparation of advanced liquid crystalline materials [ 14 , 15 ].…”

Identification of a Unique Cytotoxic Thieno[2,3-c]Pyrazole Derivative with Potent and Selective Anticancer Effects In Vitro

“…Pyrazole derivatives have been approved to treat various leukemias, lymphomas, and other cancers in the United States and China [ 3 ]. In addition, numerous experimental pyrazoles have shown antiproliferative activity and apoptosis against several cancer types in vitro [ 6 , 7 , 8 ]. In contrast, thiophene is a 5-membered heterocycle with four carbon atoms and one sulfur ( Figure 1 ).…”