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The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton

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成果类型:
期刊论文
作者:
Li, Yang;Xiao, Jie;Zhang, Qizhi;Yu, Wenmei;Liu, Mengqin;...
通讯作者:
Liu, Yunmei;He, Jun
作者机构:
[Xiao, Jie; Liu, Yunmei; Yu, Wenmei; Guo, Yu; Zhang, Qizhi; Li, Yang] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
[Liu, Mengqin] Hengyang Normal Univ, Inst Chem & Mat Sci, Hengyang 421001, Peoples R China.
通讯机构:
[Liu, Yunmei; He, Jun] U
Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
语种:
英文
关键词:
Anti-tumor;Drug target;Inhibitors of protein kinases;Quinazoline derivatives;Structure-activity relationship
期刊:
Bioorganic & Medicinal Chemistry
ISSN:
0968-0896
年:
2019
卷:
27
期:
3
页码:
568-577
基金类别:
We are grateful to the Hunan Natural Science Foundation (2018JJ2349), the University of South China Students Research Learning and Innovative Experimental Project (2018XJXZ200) and Graduate student science foundation of University of South China for financial support (2018496) for financial support.
机构署名:
本校为第一且通讯机构
院系归属:
化学化工学院
药学与生物科学学院
摘要:
Quinazoline was originally utilized as an anti-tumor treatment, and its various derivatives can be directly extracted from plants. In recent years, protein kinases (PK) have been well recognized in the development of tumor drugs. Functionally, PK serves a vital role in the apoptosis, proliferation, differentiation, migration and cell cycle of tumor cells. Due to its good physicochemical properties, quinazoline skeleton, a superior type of PK inhibitor, has been extensively used in anti-tumor drug design. An increasing number of studies on quina...

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