ReviewMolecules (Basel, Switzerland)2023
The Importance of the Pyrazole Scaffold in the Design of Protein Kinases Inhibitors as Targeted Anticancer Therapies.
Review in Molecules (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 75 citations in OpenAlex.
- Electricity-Controlled Divergent Synthesis of CFJACS Au · 2026Article
- Medicinal Chemistry of Small-Molecule c-Met Inhibitors: From Approved Therapies to Emerging Multitarget Anticancer Agents.International journal of molecular sciences · 2026Review
- Rational design of pyrazole-oxime hybrids as dual-targeting agents for glioma and breast cancer brain metastasis.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Rational Design, Synthesis, Biological Evaluation, and In Silico Study of N-Cinnamamide/Benzamide-(4-(Substituted Phenyl)-6-(4-Cyclohexylphenyl)pyrimidin-2-Yl) Derivatives as EGFR Inhibitors Targeting EGFRChemical biology & drug design · 2026Article
- Three privileged scaffolds, one pipeline: chalcones, pyrazolines and pyrazoles in drug discovery and fluorescent sensing.RSC medicinal chemistry · 2026Review
- Article
- Chemical Scaffolds Driving Modern Anticancer Drug Discovery and Radiotheranostics: Structural Determinants, Translational Opportunities and Future Perspectives.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Novel pyrazole-oxadiazole-chalcone/oxime hybrids as dual EGFR/VEGFR-2 inhibitors with promising anticancer potential: a comprehensive cytotoxicity evaluation, mechanistic insights and SAR analysis.Molecular diversity · 2026Article
- PET imaging of alpha-synuclein: from radiotracer design through in vitro and in vivo translation.European journal of nuclear medicine and molecular imaging · 2026Review
- The Pyrazole Scaffold in Anticancer Drug Discovery: A Review of Synthetic Approaches, Structure-Activity Relationships, and Target-Based Mechanism of Action.International journal of molecular sciences · 2026Review
- Article
- Pyrazole/pyrimidine derivatives endowed with azobenzenes as dual EGFRRSC advances · 2026Article
- Pyrazole in drug development: a medicinal-chemistry based analysis of USFDA-approved drugs in last decade.Molecular diversity · 2026Review
- Rationally Designed Dual Kinase Inhibitors for Management of Obstructive Sleep Apnea-A Computational Study.Biomedicines · 2026Article
- Synthesis, docking, SAR and ADMET evaluation of novel pyrrolo[3,4-c]pyrazole-4,6-dione derivatives.Scientific reports · 2026Article
- A Review of Research from 2012 to 2024 on Pyrazole-based Anticancer Agents with SAR Study.Current topics in medicinal chemistry · 2026Review
- An innovative approach to development of new pyrazolylquinolin-2-one hybrids as dual EGFR and BRAFMolecular diversity · 2025Article
- Recent Synthetic Advances in C-H/N-H Functionalization of 1H-Pyrazoles: Diverse Strategies Across Variously Substituted Scaffolds.Chemical record (New York, N.Y.) · 2025Review
- Design, Synthesis, and Evaluation of Benzoxazole-linked Pyrazole Hybrids as VEGFR-2-targeted Antiproliferative Agents.Cell biochemistry and biophysics · 2025Article
- Design, synthesis, andRSC advances · 2025Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The altered activation or overexpression of protein kinases (PKs) is a major subject of research in oncology and their inhibition using small molecules, protein kinases inhibitors (PKI) is the best available option for the cure of cancer. The pyrazole ring is extensively employed in the field of medicinal chemistry and drug development strategies, playing a vital role as a fundamental framework in the structure of various PKIs. This scaffold holds major importance and is considered a privileged structure based on its synthetic accessibility, drug-like properties, and its versatile bioisosteric replacement function. It has proven to play a key role in many PKI, such as the inhibitors of Akt, Aurora kinases, MAPK, B-raf, JAK, Bcr-Abl, c-Met, PDGFR, FGFRT, and RET. Of the 74 small molecule PKI approved by the US FDA, 8 contain a pyrazole ring: Avapritinib, Asciminib, Crizotinib, Encorafenib, Erdafitinib, Pralsetinib, Pirtobrutinib, and Ruxolitinib. The focus of this review is on the importance of the unfused pyrazole ring within the clinically tested PKI and on the additional required elements of their chemical structures. Related important pyrazole fused scaffolds like indazole, pyrrolo[1,2-b]pyrazole, pyrazolo[4,3-b]pyridine, pyrazolo[1,5-a]pyrimidine, or pyrazolo[3,4-d]pyrimidine are beyond the subject of this work.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.