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