Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors

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Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors

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dc.contributor.author Sim, Taebo
dc.contributor.author Sasaki, Takaaki
dc.contributor.author Luther, William
dc.contributor.author Deng, Xianming
dc.contributor.author Wang, Jinhua
dc.contributor.author Zhang, Jianming
dc.contributor.author Kim, Nam Doo
dc.contributor.author George, Rani E.
dc.contributor.author Jänne, Pasi A.
dc.contributor.author Gray, Nathanael Schiander
dc.date.accessioned 2012-01-03T04:10:50Z
dc.date.issued 2011
dc.identifier.citation Deng, Xianming, Jinhua Wang, Jianming Zhang, Taebo Sim, Nam Doo Kim, Takaaki Sasaki, William Luther, Rani E. George, Pasi A. Jänne, and Nathanael S. Gray. 2011. Discovery of 3,5-diamino-1,2,4-triazole ureas as potent anaplastic lymphoma kinase inhibitors. ACS Medicinal Chemistry Letters 2(5): 379-384. en_US
dc.identifier.issn 1948-5875 en_US
dc.identifier.uri http://nrs.harvard.edu/urn-3:HUL.InstRepos:5978752
dc.description.abstract A series of novel 3,5-diamino-1,2,4-triazole benzyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC50 values of 70, 40, and 20 nM in Tel-ALK transformed Ba/F3 cells, respectively. Moreover, 15a and 23a potently inhibited the growth and survival of NPM-ALK positive anaplastic large cell lymphoma cell (SU-DHL-1) and neuroblastoma cell lines (KELLY, SH-SY5Y) containing the F1174L ALK mutation. These compounds provide novel leads for the development of small-molecule ALK inhibitors for cancer therapy. en_US
dc.language.iso en_US en_US
dc.publisher American Chemical Society en_US
dc.relation.isversionof doi://10.1021/ml200002a en_US
dc.relation.hasversion http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3093683/pdf/ en_US
dash.license LAA
dc.subject ALK en_US
dc.subject 3,5-diamino-1,2,4-triazole urea en_US
dc.title Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors en_US
dc.type Journal Article en_US
dc.description.version Version of Record en_US
dc.relation.journal ACS Medicinal Chemistry Letters en_US
dash.depositing.author Gray, Nathanael Schiander
dc.date.available 2012-01-03T04:10:50Z
dash.affiliation.other HMS^Biological Chemistry and Molecular Pharmacology en_US

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