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Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors
Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC(50) values ranging from 3.2 μM to 9.9 μM) than against EGFR tyrosin...
| Autores principales: | , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Elsevier Masson SAS.
2009
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126139/ https://www.ncbi.nlm.nih.gov/pubmed/19041163 http://dx.doi.org/10.1016/j.ejmech.2008.09.051 |
| _version_ | 1783516084806090752 |
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| author | Huang, He Jia, Qi Ma, Jingui Qin, Guangrong Chen, Yingyi Xi, Yonghua Lin, Liping Zhu, Weiliang Ding, Jian Jiang, Hualiang Liu, Hong |
| author_facet | Huang, He Jia, Qi Ma, Jingui Qin, Guangrong Chen, Yingyi Xi, Yonghua Lin, Liping Zhu, Weiliang Ding, Jian Jiang, Hualiang Liu, Hong |
| author_sort | Huang, He |
| collection | PubMed |
| description | Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC(50) values ranging from 3.2 μM to 9.9 μM) than against EGFR tyrosine kinase. Molecular docking reveals that both hydrophobic and hydrogen bonding interactions are important to the selectivity. Therefore, this study provides a new promising scaffold for further development of new anticancer drugs targeting Src tyrosine kinase. |
| format | Online Article Text |
| id | pubmed-7126139 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2009 |
| publisher | Elsevier Masson SAS. |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-71261392020-04-08 Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors Huang, He Jia, Qi Ma, Jingui Qin, Guangrong Chen, Yingyi Xi, Yonghua Lin, Liping Zhu, Weiliang Ding, Jian Jiang, Hualiang Liu, Hong Eur J Med Chem Original Article Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC(50) values ranging from 3.2 μM to 9.9 μM) than against EGFR tyrosine kinase. Molecular docking reveals that both hydrophobic and hydrogen bonding interactions are important to the selectivity. Therefore, this study provides a new promising scaffold for further development of new anticancer drugs targeting Src tyrosine kinase. Elsevier Masson SAS. 2009-05 2008-10-17 /pmc/articles/PMC7126139/ /pubmed/19041163 http://dx.doi.org/10.1016/j.ejmech.2008.09.051 Text en Copyright © 2008 Elsevier Masson SAS. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active. |
| spellingShingle | Original Article Huang, He Jia, Qi Ma, Jingui Qin, Guangrong Chen, Yingyi Xi, Yonghua Lin, Liping Zhu, Weiliang Ding, Jian Jiang, Hualiang Liu, Hong Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title | Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title_full | Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title_fullStr | Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title_full_unstemmed | Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title_short | Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors |
| title_sort | discovering novel quercetin-3-o-amino acid-esters as a new class of src tyrosine kinase inhibitors |
| topic | Original Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126139/ https://www.ncbi.nlm.nih.gov/pubmed/19041163 http://dx.doi.org/10.1016/j.ejmech.2008.09.051 |
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