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10.1016/j.bmcl.2020.127613 http://scihub22266oqcxt.onion/10.1016/j.bmcl.2020.127613 33075488!7566768!33075488     free     free     free Deprecated: Implicit conversion from float 217.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 217.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 217.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 217.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 217.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Bioorg+Med+Chem+Lett 2020 ; 30 (24): 127613 Nephropedia Template TP {{tp|p=33075488|t=2020. Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers |pdf=|usr=}}{{33075488}} gab.com Text Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers JO: Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=33075488 #FOAvip 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. Twit Text FOAVip Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers ????Bioorg Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=33075488 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33075488 #FOAvip English Wikipedia <ref>{{Cite pmid|33075488}}</ref> Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers #MMPMID33075488 Chu Y; Raja Sekhara Reddy B; Pratap Reddy Gajulapalli V; Sudhakar Babu K; Kim E; Lee S Bioorg Med Chem Lett 2020[Dec]; 30 (24): 127613 PMID33075488show ga 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. |Drug Design[MESH] |Humans[MESH] |Immunity, Innate/drug effects[MESH] |Interferon Inducers/chemical synthesis/*chemistry/*pharmacology[MESH] |Interferon Type I/agonists/immunology[MESH] |Monocytes/*drug effects/immunology[MESH] |Piperazines/chemical synthesis/*chemistry/*pharmacology[MESH]Design, synthesis, and biological evaluation of N-arylpiperazine deriv(epmc).pdf DeepDyve Pubget Overpricing