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

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

Volume: 8 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Chen Shaojun, Guo Chuansheng, Shi Shiting, Shi Yanyan, Fang Du and Fan Houxing, Design, Synthesis and Pharmacokinetic Evaluation of a Novel Series of Triazole-Based Src Kinase Inhibitors with Anti-proliferative Activity, Letters in Drug Design & Discovery 2011; 8 (1) . https://dx.doi.org/10.2174/157018011793663930