Chu, Yeonjeong Reddy, B. Raja Sekhara Gajulapalli, V. Pratap Reddy Babu, K. Sudhakar Kim, Eunha Lee, Sanghee 2024-01-19T16:00:59Z 2024-01-19T16:00:59Z 2021-09-02 2020-12-15 0960-894X https://pubs.kist.re.kr/handle/201004/117682 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. English Pergamon Press Ltd. MULTIPLE-SCLEROSIS HEPATITIS DISEASES GAMMA BETA Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers Article 10.1016/j.bmcl.2020.127613 1 Bioorganic & Medicinal Chemistry Letters, v.30, no.24 Bioorganic & Medicinal Chemistry Letters 30 24 scie scopus 000595378800018 2-s2.0-85094216931 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article MULTIPLE-SCLEROSIS HEPATITIS DISEASES GAMMA BETA Interferon inducer type I Interferon Arylpiperazine Anti-viral agent Innate immunity