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Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers.

Authors
  • Chu, Yeonjeong1
  • Raja Sekhara Reddy, B2
  • Pratap Reddy Gajulapalli, V3
  • Sudhakar Babu, K4
  • Kim, Eunha5
  • Lee, Sanghee6
  • 1 Brain Science Institute, Korea Institute of Science and Technology, Seoul, South Korea; Department of Molecular Science and Technology, Ajou University, Suwon, South Korea. , (North Korea)
  • 2 Department of Chemistry, Sri Krishnadevaraya University, Anantapur, India. , (India)
  • 3 Department of Molecular Science and Technology, Ajou University, Suwon, South Korea. , (North Korea)
  • 4 Department of Chemistry, Sri Krishnadevaraya University, Anantapur, India. Electronic address: [email protected] , (India)
  • 5 Department of Molecular Science and Technology, Ajou University, Suwon, South Korea. Electronic address: [email protected] , (North Korea)
  • 6 Brain Science Institute, Korea Institute of Science and Technology, Seoul, South Korea; Department of HY-KIST Bio-convergence, Hanyang University, Seoul, South Korea. Electronic address: [email protected] , (North Korea)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Dec 15, 2020
Volume
30
Issue
24
Pages
127613–127613
Identifiers
DOI: 10.1016/j.bmcl.2020.127613
PMID: 33075488
Source
Medline
Keywords
Language
English
License
Unknown

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. Copyright © 2020 Elsevier Ltd. All rights reserved.

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