Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers
- Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers
- 이상희; 추연정; B. Raja Sekhara Reddy; V. Pratap Reddy Gajulapalli; K. Sudhakar Babu; Eunha Kim
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 30, NO 24, 127613
- 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.
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