How the structural properties of the indole derivatives are important in kinase targeted drug design?: A case study on tyrosine kinase inhibitors

التفاصيل البيبلوغرافية
العنوان: How the structural properties of the indole derivatives are important in kinase targeted drug design?: A case study on tyrosine kinase inhibitors
المؤلفون: Md. Moinul, Tarun Jha, Kalpataru Das, Sk. Abdul Amin, Shovanlal Gayen, Dipayan Mondal
المصدر: Bioorganicmedicinal chemistry. 53
سنة النشر: 2021
مصطلحات موضوعية: Indoles, Clinical Biochemistry, Druggability, Pharmaceutical Science, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, Growth factor receptor, Epidermal growth factor, Drug Discovery, Humans, Protein phosphorylation, Molecular Biology, Protein Kinase Inhibitors, Indole test, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Kinase, Organic Chemistry, Protein-Tyrosine Kinases, Cell biology, Vascular endothelial growth factor, Drug Design, Molecular Medicine, Tyrosine kinase
الوصف: Kinases are considered as important signalling enzymes that illustrate 20% of the druggable genome. Human kinase family comprises more than 500 protein kinases and about 20 lipid kinases. Protein kinases are responsible for the mechanism of protein phosphorylation. These are necessary for regulation of various cellular activities including proliferation, cell cycle, apoptosis, motility, growth, differentiation, etc. Their deregulation leads to disruption of many cellular processes leading to different diseases most importantly cancer. Thus, kinases are considered as valuable targets in different types of cancer as well as other diseases. Researchers around the world are actively engaged in developing inhibitors based on different chemical scaffolds. Indole represents as a versatile scaffold in the naturally occurring and bioactive molecules. It is also used as a privileged scaffold for the target-based drug design against different diseases. This present article aim to review the applications of indole scaffold in the design of inhibitors against different tyrosine kinases such as epidermal growth factor receptors (EGFRs), vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptor (PDGFRs), etc. Important structure activity relationships (SARs) of different indole derivatives were discussed. The present work is an attempt to summarize all the crucial structural information which is essential for the development of indole based tyrosine kinase inhibitors with improved potency.
تدمد: 1464-3391
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::031cf60e1dde4985343ecb36c1a504c0
https://pubmed.ncbi.nlm.nih.gov/34864496
Rights: OPEN
رقم الانضمام: edsair.doi.dedup.....031cf60e1dde4985343ecb36c1a504c0
قاعدة البيانات: OpenAIRE