{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,27]],"date-time":"2026-06-27T22:05:07Z","timestamp":1782597907888,"version":"3.54.5"},"reference-count":30,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2026,3,1]],"date-time":"2026-03-01T00:00:00Z","timestamp":1772323200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100010029","name":"Taishan Scholar Foundation of Shandong Province","doi-asserted-by":"publisher","award":["tsqn202408055"],"award-info":[{"award-number":["tsqn202408055"]}],"id":[{"id":"10.13039\/501100010029","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100010029","name":"Taishan Scholar Foundation of Shandong Province","doi-asserted-by":"publisher","award":["tsqn202312058"],"award-info":[{"award-number":["tsqn202312058"]}],"id":[{"id":"10.13039\/501100010029","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100007129","name":"Natural Science Foundation of Shandong Province","doi-asserted-by":"publisher","award":["ZR2023YQ066"],"award-info":[{"award-number":["ZR2023YQ066"]}],"id":[{"id":"10.13039\/501100007129","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100009108","name":"Shandong University","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100009108","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100012166","name":"National Key Research and Development Program of China","doi-asserted-by":"publisher","award":["2023YFE0206500"],"award-info":[{"award-number":["2023YFE0206500"]}],"id":[{"id":"10.13039\/501100012166","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic & Medicinal Chemistry Letters"],"published-print":{"date-parts":[[2026,3]]},"DOI":"10.1016\/j.bmcl.2025.130508","type":"journal-article","created":{"date-parts":[[2025,12,16]],"date-time":"2025-12-16T16:13:30Z","timestamp":1765901610000},"page":"130508","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":1,"special_numbering":"C","title":["Discovery and optimization of 2,3-Dihydroindole derivatives as STING receptor allosteric agonists"],"prefix":"10.1016","volume":"132","author":[{"given":"Ying","family":"Liu","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jing","family":"Wu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ni","family":"Gao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lin","family":"Zheng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenbo","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fabao","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bairu","family":"Meng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xinyong","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lanyu","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huajun","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dongwei","family":"Kang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"issue":"7780","key":"10.1016\/j.bmcl.2025.130508_bb0005","doi-asserted-by":"crossref","first-page":"691","DOI":"10.1038\/s41586-019-1605-5","article-title":"Cyclic GMP-AMP signalling protects bacteria against viral infection","volume":"574","author":"Cohen","year":"2019","journal-title":"Nature"},{"issue":"1","key":"10.1016\/j.bmcl.2025.130508_bb0010","doi-asserted-by":"crossref","first-page":"43","DOI":"10.1016\/j.immuni.2020.05.013","article-title":"Structures and mechanisms in the cGAS-STING innate immunity pathway","volume":"53","author":"Zhang","year":"2020","journal-title":"Immunity"},{"issue":"3","key":"10.1016\/j.bmcl.2025.130508_bb0015","doi-asserted-by":"crossref","first-page":"365","DOI":"10.1038\/s41589-023-01434-y","article-title":"Activation of human STING by a molecular glue-like compound","volume":"20","author":"Li","year":"2024","journal-title":"Nat Chem Biol"},{"issue":"6121","key":"10.1016\/j.bmcl.2025.130508_bb0020","doi-asserted-by":"crossref","first-page":"786","DOI":"10.1126\/science.1232458","article-title":"Cyclic GMP-AMP synthase is a cytosolic DNA sensor that activates the type I interferon pathway","volume":"339","author":"Sun","year":"2013","journal-title":"Science"},{"key":"10.1016\/j.bmcl.2025.130508_bb0025","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmc.2020.115899","article-title":"Synthesis and biological evaluation of all possible inosine-mixed cyclic dinucleotides that activate different hSTING variants","volume":"29","author":"Wang","year":"2021","journal-title":"Bioorg Med Chem"},{"issue":"8","key":"10.1016\/j.bmcl.2025.130508_bb0030","doi-asserted-by":"crossref","first-page":"4030","DOI":"10.1016\/j.apsb.2025.06.014","article-title":"Targeted inhibition of macrophage STING signaling alleviates inflammatory injury and ventricular remodeling in acute myocardial infarction","volume":"15","author":"Yao","year":"2025","journal-title":"Acta Pharm Sin B"},{"issue":"6","key":"10.1016\/j.bmcl.2025.130508_bb0035","doi-asserted-by":"crossref","first-page":"1019","DOI":"10.1016\/j.immuni.2013.10.019","article-title":"Cyclic GMP-AMP synthase is activated by double-stranded DNA-induced oligomerization","volume":"39","author":"Li","year":"2013","journal-title":"Immunity"},{"issue":"20","key":"10.1016\/j.bmcl.2025.130508_bb0040","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmcl.2019.126640","article-title":"Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy","volume":"29","author":"Ager","year":"2019","journal-title":"Bioorg Med Chem Lett"},{"issue":"7","key":"10.1016\/j.bmcl.2025.130508_bb0045","doi-asserted-by":"crossref","first-page":"1637","DOI":"10.1073\/pnas.1621363114","article-title":"cGAS is essential for the antitumor effect of immune checkpoint blockade","volume":"114","author":"Wang","year":"2017","journal-title":"Proc Natl Acad Sci USA"},{"issue":"2","key":"10.1016\/j.bmcl.2025.130508_bb0050","doi-asserted-by":"crossref","first-page":"157","DOI":"10.1016\/j.chom.2015.07.001","article-title":"STING activation by translocation from the ER is associated with infection and autoinflammatory disease","volume":"18","author":"Dobbs","year":"2015","journal-title":"Cell Host Microbe"},{"key":"10.1016\/j.bmcl.2025.130508_bb0055","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2022.114480","article-title":"Small molecules targeting cGAS-STING pathway for autoimmune disease","volume":"238","author":"Zhao","year":"2022","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.bmcl.2025.130508_bb0060","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmc.2022.116912","article-title":"Discovery of CN0 as a novel proteolysis-targeting chimera (PROTAC) degrader of PARP1 that can activate the cGAS\/STING immunity pathway combined with daunorubicin","volume":"70","author":"Lin","year":"2022","journal-title":"Bioorg Med Chem"},{"issue":"1","key":"10.1016\/j.bmcl.2025.130508_bb0065","article-title":"Precision targeting of STING: challenges, innovations, and clinical outlook for cancer therapy. The","volume":"7","author":"Shi","year":"2025","journal-title":"Innovation"},{"key":"10.1016\/j.bmcl.2025.130508_bb0070","doi-asserted-by":"crossref","first-page":"513","DOI":"10.1146\/annurev-immunol-032713-120231","article-title":"Interferon-stimulated genes: a complex web of host defenses","volume":"32","author":"Schneider","year":"2014","journal-title":"Annu Rev Immunol"},{"key":"10.1016\/j.bmcl.2025.130508_bb0075","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2020.113113","article-title":"STING, a promising target for small molecular immune modulator: a review","volume":"211","author":"Liu","year":"2021","journal-title":"Eur J Med Chem"},{"issue":"8","key":"10.1016\/j.bmcl.2025.130508_bb0080","doi-asserted-by":"crossref","first-page":"1035","DOI":"10.1038\/s41590-019-0408-z","article-title":"Interferon-\u03bb modulates dendritic cells to facilitate T cell immunity during infection with influenza a virus","volume":"20","author":"Hemann","year":"2019","journal-title":"Nat Immunol"},{"issue":"3","key":"10.1016\/j.bmcl.2025.130508_bb0085","doi-asserted-by":"crossref","first-page":"139","DOI":"10.1016\/j.it.2015.01.002","article-title":"The molecular basis for functional plasticity in type I interferon signaling","volume":"36","author":"Schreiber","year":"2015","journal-title":"Trends Immunol"},{"issue":"12","key":"10.1016\/j.bmcl.2025.130508_bb0090","doi-asserted-by":"crossref","first-page":"4765","DOI":"10.1016\/j.apsb.2023.08.015","article-title":"Non-canonical STING-PERK pathway dependent epigenetic regulation of vascular endothelial dysfunction via integrating IRF3 and NF-\u03baB in inflammatory response","volume":"13","author":"Li","year":"2023","journal-title":"Acta Pharm Sin B"},{"issue":"1","key":"10.1016\/j.bmcl.2025.130508_bb0095","doi-asserted-by":"crossref","first-page":"50","DOI":"10.1016\/j.apsb.2021.05.011","article-title":"The cGAS-STING signaling in cardiovascular and metabolic diseases: future novel target option for pharmacotherapy","volume":"12","author":"Oduro","year":"2022","journal-title":"Acta Pharm Sin B"},{"issue":"4","key":"10.1016\/j.bmcl.2025.130508_bb0100","article-title":"Novel insight into RNA modifications in tumor immunity: promising targets to prevent tumor immune escape","volume":"4","author":"Kong","year":"2023","journal-title":"Innovation (Camb)"},{"issue":"1","key":"10.1016\/j.bmcl.2025.130508_bb0105","doi-asserted-by":"crossref","first-page":"110","DOI":"10.1158\/1078-0432.CCR-22-2235","article-title":"Combination of the STING agonist MIW815 (ADU-S100) and PD-1 inhibitor Spartalizumab in advanced\/metastatic solid Tumors or lymphomas: an open-label, Multicenter","volume":"29","author":"Meric-Bernstam","year":"2023","journal-title":"Phase Ib Study Clin Cancer Res"},{"issue":"2","key":"10.1016\/j.bmcl.2025.130508_bb0110","doi-asserted-by":"crossref","DOI":"10.1136\/jitc-2024-010511","article-title":"Phase I dose-escalation and pharmacodynamic study of STING agonist E7766 in advanced solid tumors","volume":"13","author":"Luke","year":"2025","journal-title":"J Immunother Cancer"},{"issue":"7","key":"10.1016\/j.bmcl.2025.130508_bb0115","doi-asserted-by":"crossref","first-page":"5675","DOI":"10.1021\/acs.jmedchem.1c02197","article-title":"Discovery of MK-1454: a potent cyclic dinucleotide stimulator of interferon genes agonist for the treatment of Cancer","volume":"65","author":"Chang","year":"2022","journal-title":"J Med Chem"},{"issue":"12","key":"10.1016\/j.bmcl.2025.130508_bb0120","doi-asserted-by":"crossref","first-page":"2272","DOI":"10.1016\/j.apsb.2020.03.001","article-title":"Small molecules targeting the innate immune cGAS\u2013STING\u2013TBK1 signaling pathway","volume":"10","author":"Ding","year":"2020","journal-title":"Acta Pharm Sin B"},{"issue":"2","key":"10.1016\/j.bmcl.2025.130508_bb0125","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmcl.2019.126819","article-title":"Structure activity relationship, 6-modified purine riboside analogues to activate hSTING, stimulator of interferon genes","volume":"30","author":"Bonnac","year":"2020","journal-title":"Bioorg Med Chem Lett"},{"issue":"5","key":"10.1016\/j.bmcl.2025.130508_bb0130","doi-asserted-by":"crossref","first-page":"843","DOI":"10.1016\/j.immuni.2014.10.019","article-title":"STING-dependent cytosolic DNA sensing promotes radiation-induced type I interferon-dependent antitumor immunity in immunogenic Tumors","volume":"41","author":"Deng","year":"2014","journal-title":"Immunity"},{"issue":"7","key":"10.1016\/j.bmcl.2025.130508_bb0135","doi-asserted-by":"crossref","DOI":"10.3390\/molecules28072906","article-title":"Discovery of novel STING inhibitors based on the structure of the mouse STING agonist DMXAA","volume":"28","author":"Chang","year":"2023","journal-title":"Molecules"},{"issue":"7736","key":"10.1016\/j.bmcl.2025.130508_bb0140","doi-asserted-by":"crossref","first-page":"439","DOI":"10.1038\/s41586-018-0705-y","article-title":"Design of amidobenzimidazole STING receptor agonists with systemic activity","volume":"564","author":"Ramanjulu","year":"2018","journal-title":"Nature"},{"issue":"6506","key":"10.1016\/j.bmcl.2025.130508_bb0145","doi-asserted-by":"crossref","first-page":"993","DOI":"10.1126\/science.abb4255","article-title":"Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic","volume":"369","author":"Chin","year":"2020","journal-title":"Science"},{"issue":"7906","key":"10.1016\/j.bmcl.2025.130508_bb0150","doi-asserted-by":"crossref","first-page":"557","DOI":"10.1038\/s41586-022-04559-7","article-title":"Activation of STING by targeting a pocket in the transmembrane domain","volume":"604","author":"Lu","year":"2022","journal-title":"Nature"}],"container-title":["Bioorganic & Medicinal Chemistry Letters"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X25004172?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X25004172?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,14]],"date-time":"2026-05-14T20:14:13Z","timestamp":1778789653000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0960894X25004172"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,3]]},"references-count":30,"alternative-id":["S0960894X25004172"],"URL":"https:\/\/doi.org\/10.1016\/j.bmcl.2025.130508","relation":{},"ISSN":["0960-894X"],"issn-type":[{"value":"0960-894X","type":"print"}],"subject":[],"published":{"date-parts":[[2026,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery and optimization of 2,3-Dihydroindole derivatives as STING receptor allosteric agonists","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry Letters","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmcl.2025.130508","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"130508"}}