| Literature DB >> 33376012 |
Aram Faraji1, Rasoul Motahari1, Zaman Hasanvand1, Tayebeh Oghabi Bakhshaiesh2, Mahsa Toolabi3, Setareh Moghimi4, Loghman Firoozpour4, Mohammad Amin Boshagh2, Roya Rahmani2, Shima H M E Ketabforoosh5, Hamid Reza Bijanzadeh6, Rezvan Esmaeili7, Alireza Foroumadi8.
Abstract
A series of quinazolin-4(3H)-one based agents containing thiadiazole-urea were designed, synthesized, and biologically evaluated. The proliferation rate of PC3 cells was moderately reduced by compound 9f (IC50 = 17.7 μM)which was comparable with sorafenib (IC50 = 17.3 μM). There was also a significant reduction in the number of HUVEC cells, when they were exposed to compound 9y (IC50 = 6.1 μM). To test the potential of compounds in inducing apoptosis, Annexin V-FITC/propidium iodide double staining assay was used. After the treatment of HUVEC cells with 9f, they underwent apoptotic effects. A substantial effort was dedicated to gathering comprehensive data across CAM assay. These data showed that 9f moderately inhibits the growth of corresponding blood vessels. Finally, the outcomes of Western blotting proposed a mechanism of action, by which the phosphorylation of VEGFR-2 is inhibited by compounds 9f and 9y.Entities:
Keywords: Apoptotic effects; CAM assay; PC3 cells; Sorafenib; VEGFR-2; Western blotting
Year: 2020 PMID： 33376012 DOI： 10.1016/j.bioorg.2020.104553
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275