{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,20]],"date-time":"2025-10-20T00:06:33Z","timestamp":1760918793442,"version":"build-2065373602"},"reference-count":20,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2023,3,1]],"date-time":"2023-03-01T00:00:00Z","timestamp":1677628800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["82003186","82073691"],"award-info":[{"award-number":["82003186","82073691"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100021171","name":"Basic and Applied Basic Research Foundation of Guangdong Province","doi-asserted-by":"publisher","award":["2021B1515140024"],"award-info":[{"award-number":["2021B1515140024"]}],"id":[{"id":"10.13039\/501100021171","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic &amp; Medicinal Chemistry"],"published-print":{"date-parts":[[2023,3]]},"DOI":"10.1016\/j.bmc.2023.117202","type":"journal-article","created":{"date-parts":[[2023,2,10]],"date-time":"2023-02-10T21:16:56Z","timestamp":1676063816000},"page":"117202","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":0,"special_numbering":"C","title":["Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2"],"prefix":"10.1016","volume":"81","author":[{"given":"Yetong","family":"Cui","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ruonan","family":"Wang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yujiao","family":"Wei","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fei","family":"Hou","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Haixi","family":"Li","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1102-0827","authenticated-orcid":false,"given":"Yurui","family":"Jiang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yue","family":"Sun","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shushu","family":"Fu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lina","family":"Zuo","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiaoji","family":"Wang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ming","family":"Li","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jinling","family":"Li","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ning","family":"Liu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kun","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mingming","family":"Wei","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1773-9392","authenticated-orcid":false,"given":"Guang","family":"Yang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmc.2023.117202_b0005","first-page":"87","article-title":"Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries","volume":"65","author":"Sung","year":"2021","journal-title":"CA Cancer J Clin"},{"key":"10.1016\/j.bmc.2023.117202_b0010","doi-asserted-by":"crossref","first-page":"584","DOI":"10.1016\/S0025-6196(11)60735-0","article-title":"Non-small cell lung cancer: epidemiology, risk factors, treatment, and survivorship","volume":"83","author":"Molina","year":"2008","journal-title":"Mayo Clin Proc"},{"key":"10.1016\/j.bmc.2023.117202_b0015","doi-asserted-by":"crossref","first-page":"446","DOI":"10.1038\/nature25183","article-title":"The biology and management of nonsmall cell lung cancer","volume":"553","author":"Herbst","year":"2018","journal-title":"Nature"},{"key":"10.1016\/j.bmc.2023.117202_b0020","doi-asserted-by":"crossref","first-page":"239","DOI":"10.1016\/S1470-2045(11)70393-X","article-title":"Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial","volume":"13","author":"Rosell","year":"2012","journal-title":"Lancet Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0025","doi-asserted-by":"crossref","first-page":"2240","DOI":"10.1158\/1078-0432.CCR-12-2246","article-title":"Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers","volume":"19","author":"Yu","year":"2013","journal-title":"Clin Cancer Res"},{"key":"10.1016\/j.bmc.2023.117202_b0030","doi-asserted-by":"crossref","first-page":"2129","DOI":"10.1056\/NEJMoa040938","article-title":"Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib","volume":"350","author":"Lynch","year":"2004","journal-title":"N Engl J Med"},{"key":"10.1016\/j.bmc.2023.117202_b0035","doi-asserted-by":"crossref","first-page":"1817","DOI":"10.1111\/j.1349-7006.2007.00607.x","article-title":"Mutations of the epidermal growth factor receptor gene and related genes as determinants of epidermal growth factor receptor tyrosine kinase inhibitors sensitivity in lung cancer","volume":"98","author":"Mitsudomi","year":"2007","journal-title":"Cancer Sci"},{"key":"10.1016\/j.bmc.2023.117202_b0040","doi-asserted-by":"crossref","first-page":"179","DOI":"10.1097\/JTO.0b013e3182779d18","article-title":"Natural history and molecular characteristics of lung cancers harboring EGFR Exon 20 insertions","volume":"8","author":"Oxnard","year":"2013","journal-title":"J Thorac Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0045","doi-asserted-by":"crossref","first-page":"216ra177","DOI":"10.1126\/scitranslmed.3007205","article-title":"Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer","volume":"5","author":"Yasuda","year":"2013","journal-title":"Sci Transl Med"},{"key":"10.1016\/j.bmc.2023.117202_b0050","doi-asserted-by":"crossref","first-page":"e23","DOI":"10.1016\/S1470-2045(11)70129-2","article-title":"EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications","volume":"13","author":"Yasuda","year":"2012","journal-title":"Lancet Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0055","doi-asserted-by":"crossref","first-page":"220","DOI":"10.1158\/1535-7163.MCT-12-0620","article-title":"EGFR exon 20 insertion mutations in lung adenocarcinomas: prevalence, molecular heterogeneity, and clinicopathologic characteristics","volume":"12","author":"Arcila","year":"2013","journal-title":"Mol Cancer Ther"},{"key":"10.1016\/j.bmc.2023.117202_b0060","doi-asserted-by":"crossref","first-page":"171","DOI":"10.1002\/ijc.30047","article-title":"NSCLC harboring EGFR exon-20 insertions after the regulatory C-helix of kinase domain responds poorly to known EGFR inhibitors","volume":"139","author":"Yang","year":"2016","journal-title":"Int J Cancer"},{"key":"10.1016\/j.bmc.2023.117202_b0065","doi-asserted-by":"crossref","first-page":"7634","DOI":"10.1002\/anie.201703389","article-title":"Discovery of EGF receptor inhibitors that are selective for the d746\u2013750\/T790M\/C797S mutant through structure-based de novo design","volume":"56","author":"Park","year":"2017","journal-title":"Angew Chem Int Ed"},{"key":"10.1016\/j.bmc.2023.117202_b0070","doi-asserted-by":"crossref","first-page":"4910","DOI":"10.1158\/1078-0432.CCR-12-0912","article-title":"Prevalence, clinicopathologic associations, and molecular spectrum of ERBB2 (HER2) tyrosine kinase mutations in lung adenocarcinomas","volume":"18","author":"Arcila","year":"2012","journal-title":"Clin Cancer Res"},{"key":"10.1016\/j.bmc.2023.117202_b0075","doi-asserted-by":"crossref","first-page":"1997","DOI":"10.1200\/JCO.2012.45.6095","article-title":"Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives","volume":"31","author":"Mazieres","year":"2013","journal-title":"J Clin Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0080","doi-asserted-by":"crossref","first-page":"S1536","DOI":"10.1016\/j.jtho.2017.06.020","article-title":"Preliminary results of a phase II study of Poziotinib in EGFR exon 20 mutant advanced NSCLC","volume":"12","author":"Elamin","year":"2017","journal-title":"J Thorac Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0085","doi-asserted-by":"crossref","first-page":"S323","DOI":"10.1016\/j.jtho.2018.08.243","article-title":"A phase II trial of poziotinib in EGFR and HER2 exon 20 mutant non-small cell lung cancer (NSCLC)","volume":"13","author":"Heymach","year":"2021","journal-title":"J. Thora. Oncol."},{"key":"10.1016\/j.bmc.2023.117202_b0090","doi-asserted-by":"crossref","first-page":"S815","DOI":"10.1016\/j.annonc.2020.08.1575","article-title":"Updated results from a phase I\/II study of mobocertinib (TAK788) in NSCLC with EGFR exon 20 insertions (exon20ins)","volume":"31","author":"Riely","year":"2020","journal-title":"Ann Oncol"},{"key":"10.1016\/j.bmc.2023.117202_b0095","doi-asserted-by":"crossref","first-page":"1672","DOI":"10.1158\/2159-8290.CD-20-1683","article-title":"Mobocertinib (TAK-788): a targeted inhibitor of EGFR Exon 20 insertion mutants in non-small cell lung cancer","volume":"11","author":"Gonzalvez","year":"2021","journal-title":"Cancer Discov"},{"key":"10.1016\/j.bmc.2023.117202_b0100","doi-asserted-by":"crossref","first-page":"S359","DOI":"10.1016\/j.jtho.2016.11.399","article-title":"MA04.03 preliminary results of a phase ii study about the efficacy and safety of pyrotinib in patients with HER2 mutant advanced NSCLC","volume":"12","author":"Ren","year":"2017","journal-title":"J Thorac Oncol"}],"container-title":["Bioorganic &amp; Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089623000500?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0968089623000500?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,19]],"date-time":"2025-10-19T01:21:43Z","timestamp":1760836903000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0968089623000500"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2023,3]]},"references-count":20,"alternative-id":["S0968089623000500"],"URL":"https:\/\/doi.org\/10.1016\/j.bmc.2023.117202","relation":{},"ISSN":["0968-0896"],"issn-type":[{"type":"print","value":"0968-0896"}],"subject":[],"published":{"date-parts":[[2023,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmc.2023.117202","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2023 Elsevier Ltd. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"117202"}}