Synthesis and Biological Evaluation of Glycyrrhetic Acid Derivatives as Potential VEGFR2 Inhibitors.

Synthesis and Biological Evaluation of Glycyrrhetic Acid Derivatives as Potential VEGFR2 Inhibitors.

ChemMedChem. 2017 Jun 09;:

Authors: Lv P, Yan TL, Bai LF, Zhu HL, Zhang WM

Abstract
Vascular endothelial growth factor receptor 2 (VEGFR2) has been proven to play a major role in the regulation of tumor angiogenesis. A series of novel glycyrrhetic acid derivatives have been synthesized and evaluated for their VEGFR2 inhibitory activity as well as their antiproliferative properties against four cancer cell lines (MCF-7, Hela, HepG2 and A549). In vitro biological evaluation against four human tumor cell lines indicated that most of the prepared compounds showed antiproliferative activities, and compound 3a exhibited the best inhibitory activity against MCF-7 with the IC50 value of 1.08 μM. Also, compound 3a showed the most potent inhibitory activities against VEGFR2 tyrosine kinase with the IC50 value of 0.35 μM. A docking simulation study was performed with the aim of discovering the binding mode of compound 3a, and the result showed that compound 3a could bind well at the VEGFR2 active site.

PMID: 28599090 [PubMed - as supplied by publisher]

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