294851-80-2Relevant academic research and scientific papers
Quinazolin-4(3H)-one based agents bearing thiadiazole-urea: Synthesis and evaluation of anti-proliferative and antiangiogenic activity
Faraji, Aram,Motahari, Rasoul,Hasanvand, Zaman,Oghabi Bakhshaiesh, Tayebeh,Toolabi, Mahsa,Moghimi, Setareh,Firoozpour, Loghman,Boshagh, Mohammad Amin,Rahmani, Roya,Ketabforoosh, Shima H.M.E.,Bijanzadeh, Hamid Reza,Esmaeili, Rezvan,Foroumadi, Alireza
, (2021)
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.
Design, synthesis and evaluation of novel thienopyrimidine-based agents bearing diaryl urea functionality as potential inhibitors of angiogenesis
Faraji, Aram,Oghabi Bakhshaiesh, Tayebeh,Hasanvand, Zaman,Motahari, Rasoul,Nazeri, Elahe,Boshagh, Mohammad Amin,Firoozpour, Loghman,Mehrabi, Hossein,Khalaj, Ali,Esmaeili, Rezvan,Foroumadi, Alireza
, (2020/10/27)
Inhibition of angiogenesis is a promising strategy for the treatment of cancer. Herein, we describe the design and synthesis of thieno[2,3-d]pyrimidine-1,3,4-thiadiazole-aryl urea derivatives 11a-m to evaluate their efficacy in the chick chorioallantoic membrane (CAM) assay. Among target agents, 11i had a considerable activity against prostate cancer cell line, PC3 (IC50 = 3.6 μM). Moreover, induction of apoptosis, good inhibitory activity against the growth of capillary blood vessels, and inhibition of VEGFR-2 phosphorylation were noticeable parameters which convinced us that 11i could be considered as a promising candidate for the discovery of novel drugs to treat tumors, particularly prostate cancer.
