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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
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Genetics Department, Breast Cancer Research Center, Motamed Cancer Institute, ACECR, Tehran, Iran
  3. 3. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Chemistry, Vali-e-Asr University of Rafsanjan, Rafsanjan, 77176, Iran

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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