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Design, Synthesis, in Vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-A]Pyridines As Potent Anti-Breast Cancer Agents Publisher Pubmed



Khalili F1 ; Akrami S2 ; Safavi M3 ; Mohammadikhanaposhtani M4 ; Saeedi M5, 6 ; Ardestani SK1 ; Larijani B7 ; Zonouzi A2 ; Tehrani MB8 ; Mahdavi M7
Authors
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Authors Affiliations
  1. 1. Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran
  2. 2. School of Chemistry, College of Science, University of Tehran, Tehran, Iran
  3. 3. Department of Biotechnology, Iranian Research Organization for Science and Technology (IROST), Tehran, Iran
  4. 4. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  5. 5. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  7. 7. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  8. 8. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Anti-Cancer Agents in Medicinal Chemistry Published:2019


Abstract

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents. © 2019 Bentham Science Publishers.
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