Design, Synthesis and Pharmacokinetic Evaluation of a Novel Series of Triazole-Based Src Kinase Inhibitors with Anti-proliferative Activity

Author(s): Shaojun Chen, Chuansheng Guo, Shiting Shi, Yanyan Shi, Du Fang, Houxing Fan.

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 1 , 2011

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Abstract:

Src has been recognized as an important therapeutic target for the treatment of cancer. A novel series of triazole- based Src inhibitors were synthesized and evaluated for their anti-proliferative activities in vitro against human lung cancer A549 cells with Bosutinib as reference compound, most of the compounds showed more potent activity than Bosutinib. Compounds 6 and 8 were further subjected to pharmacokinetic performance assessment, both the compounds displayed low plasma concentrations and short half-time.

Keywords: Anti-proliferative activity, Biological activity, SKI-606, Src Kinase, Synthesis, Triazoly group, Src, cancer, A549 cells, Bosutinib, tyrosine kinase, tumorigenesis, metastasis, tissue invasion, osteoporosis, myocardial infarction, Dasatinib, Saracatinib, VEGFRr TK, analogues, TMS-Acetylene, HNMR, MTT, DMSO, IC50, pharmacokinetic, AUC, PK

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Article Details

VOLUME: 8
ISSUE: 1
Year: 2011
Page: [9 - 13]
Pages: 5
DOI: 10.2174/157018011793663930

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