1. Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors
- Author
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Huang, He, Jia, Qi, Ma, Jingui, Qin, Guangrong, Chen, Yingyi, Xi, Yonghua, Lin, Liping, Zhu, Weiliang, Ding, Jian, Jiang, Hualiang, and Liu, Hong
- Subjects
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DRUG development , *PROTEIN-tyrosine kinase inhibitors , *QUERCETIN , *ESTERS , *AMINO acids , *HYDROGEN bonding , *PHARMACEUTICAL chemistry , *TARGETED drug delivery - Abstract
Abstract: 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 (IC50 values ranging from 3.2μM to 9.9μM) 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. [Copyright &y& Elsevier]
- Published
- 2009
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