{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,1]],"date-time":"2025-10-01T16:35:36Z","timestamp":1759336536205,"version":"build-2065373602"},"reference-count":28,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2019,9,1]],"date-time":"2019-09-01T00:00:00Z","timestamp":1567296000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2019,9,1]],"date-time":"2019-09-01T00:00:00Z","timestamp":1567296000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2019,9]]},"DOI":"10.1016\/j.ejmech.2019.05.091","type":"journal-article","created":{"date-parts":[[2019,6,3]],"date-time":"2019-06-03T13:23:36Z","timestamp":1559568216000},"page":"232-242","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":5,"special_numbering":"C","title":["Discovery of novel Bcr-AblT315I inhibitors with flexible linker. Part 1: Confirmation optimization of phenyl-1H-indazol-3-amine as hinge binding moiety"],"prefix":"10.1016","volume":"178","author":[{"given":"Xiaoyan","family":"Pan","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Liyuan","family":"Liang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ying","family":"Sun","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ru","family":"Si","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qingqing","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jin","family":"Wang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jia","family":"Fu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Junjie","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2727-8806","authenticated-orcid":false,"given":"Jie","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2019.05.091_bib1","doi-asserted-by":"crossref","first-page":"3530","DOI":"10.1182\/blood.V99.10.3530","article-title":"Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study","volume":"99","author":"Sawyers","year":"2002","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2019.05.091_bib2","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1038\/nrc3563","article-title":"Role of ABL family kinases in cancer: from leukaemia to solid tumors","volume":"13","author":"Greuber","year":"2013","journal-title":"Nat. Rev. Canc."},{"key":"10.1016\/j.ejmech.2019.05.091_bib3","doi-asserted-by":"crossref","first-page":"1619","DOI":"10.1182\/blood-2008-03-144790","article-title":"Molecular biology of bcr-abl1-positive chronic myeloid leukemia","volume":"113","author":"Quintas-Cardama","year":"2009","journal-title":"Blood"},{"key":"10.1016\/j.ejmech.2019.05.091_bib4","doi-asserted-by":"crossref","first-page":"493","DOI":"10.1038\/nrd839","article-title":"Glivec (STI571, Imatinib), a rationally developed, targeted anticancer drug","volume":"1","author":"Capdeville","year":"2002","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2019.05.091_bib5","doi-asserted-by":"crossref","first-page":"220","DOI":"10.1016\/j.canlet.2016.09.025","article-title":"PBA2, a novel inhibitor of imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia","volume":"383","author":"Gupta","year":"2016","journal-title":"Cancer Lett."},{"key":"10.1016\/j.ejmech.2019.05.091_bib6","doi-asserted-by":"crossref","first-page":"S3","DOI":"10.1053\/j.seminoncol.2011.01.016","article-title":"Nilotinib: a novel, selective tyrosine kinase inhibitor","volume":"38","author":"Blay","year":"2011","journal-title":"Semin. Oncol."},{"key":"10.1016\/j.ejmech.2019.05.091_bib7","doi-asserted-by":"crossref","first-page":"399","DOI":"10.1126\/science.1099480","article-title":"Overriding imatinib resistance with a novel ABL kinase inhibitor","volume":"305","author":"Shah","year":"2004","journal-title":"Science"},{"key":"10.1016\/j.ejmech.2019.05.091_bib8","doi-asserted-by":"crossref","first-page":"1703","DOI":"10.1177\/1060028013503124","article-title":"Bosutinib: a second-generation tyrosine kinase inhibitor for chronic myelogenous leukemia","volume":"47","author":"Stansfield","year":"2013","journal-title":"Ann. Pharmacother."},{"key":"10.1016\/j.ejmech.2019.05.091_bib9","doi-asserted-by":"crossref","first-page":"6948","DOI":"10.1038\/srep06948","article-title":"Identification of novel tyrosine kinase inhibitors for drug resistant T315I mutant BCR-ABL: a virtual screening and molecular dynamics simulations study","volume":"4","author":"Banayath","year":"2014","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2019.05.091_bib10","doi-asserted-by":"crossref","first-page":"401","DOI":"10.1016\/j.ccr.2009.09.028","article-title":"AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance","volume":"16","author":"O'Hare","year":"2009","journal-title":"Cancer Cell"},{"author":"U.S. Food and Drug Administration","key":"10.1016\/j.ejmech.2019.05.091_bib11"},{"key":"10.1016\/j.ejmech.2019.05.091_bib12","doi-asserted-by":"crossref","first-page":"779","DOI":"10.1016\/j.chembiol.2006.05.015","article-title":"A\u00a0general strategy for creating \u201cinactive-confirmation\u201d abl inhibitors","volume":"13","author":"Okram","year":"2006","journal-title":"Chem. Biol."},{"key":"10.1016\/j.ejmech.2019.05.091_bib13","doi-asserted-by":"crossref","first-page":"7050","DOI":"10.1039\/C5OB00430F","article-title":"Discovery of novel Bcr-abl inhibitors with diacylated piperazine as the flexible linker","volume":"13","author":"Pan","year":"2015","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib14","doi-asserted-by":"crossref","first-page":"911","DOI":"10.1007\/s00280-011-1740-7","article-title":"A\u00a0novel multi-targeted tyrosine kinase inhibitor, linifanib (ABT-869), produces functional and structural changes in tumor vasculature in an orthotopic rat glioma model","volume":"69","author":"Luo","year":"2012","journal-title":"Cancer Chemother. Pharmacol."},{"key":"10.1016\/j.ejmech.2019.05.091_bib15","doi-asserted-by":"crossref","first-page":"139","DOI":"10.1016\/j.ejmech.2015.09.034","article-title":"Expanding the structural diversity of Bcr-Abl inhibitors: dibenzoylpiperazin incorporated with 1H-indazol-3-amine","volume":"104","author":"Shan","year":"2015","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib16","doi-asserted-by":"crossref","first-page":"1419","DOI":"10.1021\/op900208y","article-title":"The discovery and development of a safe, practical synthesis of ABT-869, Org","volume":"13","author":"Kruger","year":"2009","journal-title":"Process Res. Dev."},{"key":"10.1016\/j.ejmech.2019.05.091_bib17","doi-asserted-by":"crossref","first-page":"1943","DOI":"10.1002\/adsc.201701641","article-title":"Lewis-acid promoted chemoselective condensation of 2-aminobenzimi-dazoles or 3-aminoindazoles with 3-ethoxycyclo-butanones to construct fused nitrogen heterocycles","volume":"360","author":"Kong","year":"2018","journal-title":"Adv. Synth. Catal."},{"key":"10.1016\/j.ejmech.2019.05.091_bib18","doi-asserted-by":"crossref","first-page":"326","DOI":"10.1039\/C1GC16314K","article-title":"CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines","volume":"14","author":"Verma","year":"2012","journal-title":"Green Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib19","doi-asserted-by":"crossref","first-page":"2485","DOI":"10.1021\/ol016107o","article-title":"Facile synthesis of rotaxanes through condensation reactions of DCC-[2]rotaxanes","volume":"3","author":"2nd Zehnder","year":"2001","journal-title":"Org. Lett."},{"key":"10.1016\/j.ejmech.2019.05.091_bib20","doi-asserted-by":"crossref","first-page":"361","DOI":"10.1055\/s-2001-11425","article-title":"Reaction of piperazine with trimethylacetic arylcarboxylic anhydride; A convenient method for preparing monoacylated piperazine derivatives","volume":"3","author":"Lai","year":"2001","journal-title":"Synthesis"},{"key":"10.1016\/j.ejmech.2019.05.091_bib21","doi-asserted-by":"crossref","first-page":"2527","DOI":"10.1016\/j.bmc.2013.02.036","article-title":"Design, synthesis and biological activities of Nilotinib derivates as antitumor agents","volume":"21","author":"Pan","year":"2013","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib22","doi-asserted-by":"crossref","first-page":"560","DOI":"10.1089\/adt.2009.0222","article-title":"ADP-Glo: a Bioluminescent and homogeneous ADP monitoring assay for kinases","volume":"7","author":"Zegzouti","year":"2009","journal-title":"Assay Drug Dev. Technol."},{"key":"10.1016\/j.ejmech.2019.05.091_bib23","doi-asserted-by":"crossref","first-page":"780","DOI":"10.1016\/j.ejmech.2015.07.015","article-title":"Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents","volume":"101","author":"Dong","year":"2015","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib24","doi-asserted-by":"crossref","first-page":"28352","DOI":"10.1038\/srep28352","article-title":"The chimeric ubiquitin ligase SH2-U-box inhibits the growth of imatinib-sensitive and resistant CML by targeting the native and T315I-mutant BCR-ABL","volume":"6","author":"Ru","year":"2016","journal-title":"Sci. Rep."},{"key":"10.1016\/j.ejmech.2019.05.091_bib25","doi-asserted-by":"crossref","first-page":"750","DOI":"10.1016\/j.ejmech.2013.10.047","article-title":"Synthesis, biological evaluation and docking studies of 4-aryloxymethyl coumarins derived from substructures and degradation products of vancomycin","volume":"70","author":"Revankar","year":"2013","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2019.05.091_bib26","first-page":"4236","article-title":"Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571)","volume":"62","author":"Nagar","year":"2002","journal-title":"Cancer Res."},{"key":"10.1016\/j.ejmech.2019.05.091_bib27","doi-asserted-by":"crossref","first-page":"556","DOI":"10.1016\/j.ccr.2011.03.003","article-title":"Conformational control inhibition of the BCR-ABL 1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036","volume":"19","author":"Chan","year":"2011","journal-title":"Cancer Cell"},{"key":"10.1016\/j.ejmech.2019.05.091_bib28","doi-asserted-by":"crossref","first-page":"12102","DOI":"10.1021\/jacs.8b06738","article-title":"Cell-permeable bicyclic peptidyl inhibitors against NEMO-I\u03baB kinase interaction directly from a combinatorial library","volume":"140","author":"Rhodes","year":"2018","journal-title":"J.\u00a0Am. Chem. Soc."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S022352341930515X?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S022352341930515X?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,1]],"date-time":"2025-10-01T13:55:49Z","timestamp":1759326949000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S022352341930515X"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2019,9]]},"references-count":28,"alternative-id":["S022352341930515X"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2019.05.091","relation":{},"ISSN":["0223-5234"],"issn-type":[{"type":"print","value":"0223-5234"}],"subject":[],"published":{"date-parts":[[2019,9]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of novel Bcr-AblT315I inhibitors with flexible linker. Part 1: Confirmation optimization of phenyl-1H-indazol-3-amine as hinge binding moiety","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2019.05.091","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2019 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}]}}