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Design, Synthesis and Evaluation of Novel Thienopyrimidine-Based Agents Bearing Diaryl Urea Functionality As Potential Inhibitors of Angiogenesis Publisher Pubmed



Faraji A1 ; Oghabi Bakhshaiesh T2 ; Hasanvand Z1 ; Motahari R1 ; Nazeri E2 ; Boshagh MA2 ; Firoozpour L3 ; Mehrabi H4 ; Khalaj A1 ; Esmaeili R2 ; Foroumadi A1, 3
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Source: European Journal of Medicinal Chemistry Published:2021


Abstract

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. © 2020 Elsevier Masson SAS
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