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Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducersoa mark
  • Chu, Yeonjeong ;
  • Raja Sekhara Reddy, B. ;
  • Pratap Reddy Gajulapalli, V. ;
  • Sudhakar Babu, K. ;
  • Kim, Eunha ;
  • Lee, Sanghee
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Publication Year
2020-12-15
Journal
Bioorganic and Medicinal Chemistry Letters
Publisher
Elsevier Ltd
Citation
Bioorganic and Medicinal Chemistry Letters, Vol.30 No.24
Keyword
Anti-viral agentArylpiperazineInnate immunityInterferon inducertype I Interferon
Mesh Keyword
Drug DesignHumansImmunity, InnateInterferon InducersInterferon Type IMonocytesPiperazinesTHP-1 Cells
All Science Classification Codes (ASJC)
BiochemistryMolecular MedicineMolecular BiologyPharmaceutical ScienceDrug DiscoveryClinical BiochemistryOrganic Chemistry
Abstract
Type I Interferon (IFN) signaling plays an important role in the immune defense system against virus infection and in the innate immune response, thus IFNs are widely used as anti-viral agents and treatment for immune disorder or cancer. However, there is a growing demand for novel small-molecule IFN inducer due to tolerance, toxicity, or short duration of action following direct administration of IFNs. In this study, we assessed arylpiperazine (ARP) as a new core skeleton of IFN inducer. To investigate structure–activity relationship, we designed and synthesized a series of ARP analogues and evaluated the ability to stimulate IFN response in THP-1 human monocyte cells. Compound 5i was identified as a potent type I IFN inducer as it significantly increased cytokine secretion and increased expression of various IFN-stimulating genes which are representative biomarkers of type I IFN pathway. Our results suggested a beneficial therapeutic potential of 5i as an anti-viral agent.
ISSN
1464-3405
Language
eng
URI
https://aurora.ajou.ac.kr/handle/2018.oak/31636
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85094216931&origin=inward
DOI
https://doi.org/10.1016/j.bmcl.2020.127613
Journal URL
http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry-letters/
Type
Article
Funding
This study was financially supported by Korea Institute of Science and Technology (KIST) Institutional Program (2E30180) and Bio & Medical Technology Development Program (NRF-2019M3E5D4066905) of the National Research Foundation funded by Korean government (MSIT), a grant from Priority Research Centers Program (2019R1A6A1A11051471), 2020R1C1C1010044 funded by the National Research Foundation of Korea (NRF) and Convergence brain research through cross-institute collaboration (KBRI 20-BR-03-01/ IBS-R001-D1-2020-b02).This study was financially supported by Korea Institute of Science and Technology (KIST) Institutional Program (2E30180) and Bio & Medical Technology Development Program (NRF-2019M3E5D4066905) of the National Research Foundation funded by Korean government (MSIT), a grant from Priority Research Centers Program (2019R1A6A1A11051471), 2020R1C1C1010044 funded by the National Research Foundation of Korea (NRF) and Convergence brain research through cross-institute collaboration (KBRI 20-BR-03-01/ IBS-R001-D1-2020-b02).
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Kim, Eun ha김은하
College of Bio-convergence Engineering
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