[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update

R Roskoski Jr - Pharmacological research, 2024 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

Recent advances in the development of pyrazole derivatives as anticancer agents

Y Zhang, C Wu, N Zhang, R Fan, Y Ye, J Xu - International Journal of …, 2023 - mdpi.com
Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical
structures that confer them with a broad spectrum of pharmacological activities. They have …

Recent advances in the synthesis of pyrazole derivatives: a review

I Ameziane El Hassani, K Rouzi, H Assila, K Karrouchi… - Reactions, 2023 - mdpi.com
Pyrazole, characterized by a five-membered heterocyclic structure featuring two neighboring
nitrogen atoms, serves as a core element. Pyrazoles hold a privileged status as versatile …

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

A Mushtaq, P Wu, MM Naseer - Pharmacology & Therapeutics, 2023 - Elsevier
Cancer, a noncommunicable disease, is the leading cause of mortality worldwide and is
anticipated to rise by 75% in the next two decades, reaching approximately 25 million cases …

A novel class of pyrazole analogues as Aurora kinase a inhibitor: design, synthesis, and anticancer evaluation

DB Yevale, N Teraiya, TD Lalwani, RK Ameta… - Bioorganic …, 2023 - Elsevier
Pyrazole, as a small molecule, was discovered for higher cytotoxicity and affinity towards
Aurora-A kinase. Based on these facts, a novel pyrazole substituted at the 4 th position was …

[HTML][HTML] Synthesis, antitumor Activity, antimicrobial evaluation and molecular docking studies of some Hydrazone, 1, 3, 4-Oxadiazole, 1, 2, 4-Triazole and pyrazole …

AR Farghaly, SA Ahmed, KS Ismail, D Ibrahim… - Results in …, 2024 - Elsevier
In this study, we synthesized a number of new intriguing azoles bearing nicotinoyl moiety,
their antimicrobial and antitumor activities were investigated as well. We succeeded to …

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

M Lusardi, MG Signorello, E Russo, D Caviglia… - International Journal of …, 2024 - mdpi.com
Aminopyrazoles represent interesting structures in medicinal chemistry, and several
derivatives showed biological activity in different therapeutic areas. Previously reported 5 …

Inhibition of human epidermal growth factor receptor-2 protein by some alkaloid inhibitors

L Razavi, H Raissi - Journal of Molecular Liquids, 2024 - Elsevier
Abstract Background Human Epidermal Growth Factor Receptor-2 (HER2), a
transmembrane tyrosine kinase receptor, has been associated with several types of cancer …

Development of 1, 5-diarylpyrazoles as EGFR/JNK-2 dual inhibitors: design, synthesis, moleecular docking, and bioactivity evaluation

OM Soltan, SA Abdel-Aziz, MS Shaykoon… - Bioorganic & Medicinal …, 2024 - Elsevier
The eradication of multifactorial diseases, such as cancer, requires the design of drug
candidates that attack multiple targets that contribute to the progression and proliferation of …

Exploring chemical space, scaffold diversity, and activity landscape of spleen tyrosine kinase active inhibitors

Danishuddin, MZ Malik, M Kashif… - SAR and QSAR in …, 2024 - Taylor & Francis
This study aims to comprehensively characterize 576 inhibitors targeting Spleen Tyrosine
Kinase (SYK), a non-receptor tyrosine kinase primarily found in haematopoietic cells, with …