| Literature DB >> 26920800 |
Zhao Yang1, Zheng Fang2, Wei He3, Zhixiang Wang1, Haifeng Gan3, Qitao Tian3, Kai Guo3.
Abstract
The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reacting aldehydes with amines. Four sensitive binders targeted VEGFR-2 were directly isolated from the library. Antitumor activity test in vitro and inhibition experiments toward angiogenesis were also carried out.Entities:
Keywords: Drug discovery; Dynamic combinatorial chemistry; Enzyme inhibitors; Imine formation; Ligand separation
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Year: 2016 PMID： 26920800 DOI： 10.1016/j.bmcl.2016.02.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823