Research paperSynthesis and biological evaluation as antiangiogenic agents of ureas derived from 3′-aminocombretastatin A-4

Add time:08/22/2019    Source:sciencedirect.com

Twenty-six compounds derived from 3′-aminocombretastatin A-4 (AmCA-4) containing a urea fragment mimicking the structure of Sorafenib, have been synthesized and evaluated as antiangiogenic compounds. Antiproliferative activity of all the synthetic ureas has been measured on tumor cell lines HT-29, MCF-7, HeLa, A-549 and HL-60 as well as on the endothelial cell line HMEC-1 and on the non-tumor cell line HEK-293. Preliminary docking studies were developed in order to predict which ureas show better interactions with the protein VEGFR-2. Then, the selected derivatives were evaluated in terms of their apoptotic effect and antiangiogenic properties. In this regard, VEGFR-2/ligand interactions were determined by flow cytometry and immunofluorescence techniques. Inhibition of VEGFR-2 tyrosine kinase activity in both the A-549 and HMEC-1 cell lines was also carried out. In addition, tube formation inhibition was studied in endothelial cells. Ortho-chloro substituted urea 5 and ortho-bromo substituted urea 8 were the most active ones in both down-regulation of VEGFR-2 and inhibition of the kinase activity of this receptor, with better results than those obtained with sunitinib and sorafenib.

We also recommend Trading Suppliers and Manufacturers of N-(3,4-DIMETHYLPHENYL)UREA (cas 114-79-4). Pls Click Website Link as below: cas 114-79-4 suppliers

Prev:Phenylalanine and phenylpyruvate inhibit ATP diphosphohydrolase from rat brain cortex
Next:Original articleSynthesis and anti-inflammatory evaluation of some condensed [4-(3,4-dimethylphenyl)-1(2H)-oxo-phthalazin-2-yl]acetic acid hydrazide)