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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2007-4-30
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pubmed:abstractText |
Novel C-5 aminomethyl pyrrolotriazines were prepared and optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The homopiperazine, 1p, emerged as a key lead and it showed promising oral efficacy in EGFR and dual EGFR/HER2 driven human tumor xenograft models. It is hypothesized that the C-5 homopiperazine side chain binds in the ribose-phosphate portion of the ATP binding pocket.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ChangMingM,
pubmed-author:GavaiAshvinikumarA,
pubmed-author:JohnsonWalterW,
pubmed-author:LangleyDavidD,
pubmed-author:LeeFrancis YFY,
pubmed-author:MarathePunitP,
pubmed-author:MastalerzHaroldH,
pubmed-author:MathurArvindA,
pubmed-author:OppenheimerSimoneS,
pubmed-author:TarrantJamesJ,
pubmed-author:TokarskiJohn SJS,
pubmed-author:ViteGregory DGD,
pubmed-author:VyasDolatrai MDM,
pubmed-author:WongHenryH,
pubmed-author:WongTai WTW,
pubmed-author:ZhangGuifenG,
pubmed-author:ZhangHongjianH
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2828-33
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17368025-Animals,
pubmed-meshheading:17368025-Antineoplastic Agents,
pubmed-meshheading:17368025-Cell Line, Tumor,
pubmed-meshheading:17368025-Disease Models, Animal,
pubmed-meshheading:17368025-Drug Screening Assays, Antitumor,
pubmed-meshheading:17368025-Humans,
pubmed-meshheading:17368025-Methylamines,
pubmed-meshheading:17368025-Mice,
pubmed-meshheading:17368025-Models, Molecular,
pubmed-meshheading:17368025-Molecular Structure,
pubmed-meshheading:17368025-Neoplasm Transplantation,
pubmed-meshheading:17368025-Protein-Tyrosine Kinases,
pubmed-meshheading:17368025-Pyrroles,
pubmed-meshheading:17368025-Receptor, Epidermal Growth Factor,
pubmed-meshheading:17368025-Receptor, erbB-2,
pubmed-meshheading:17368025-Structure-Activity Relationship,
pubmed-meshheading:17368025-Triazines,
pubmed-meshheading:17368025-Xenograft Model Antitumor Assays
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pubmed:year |
2007
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pubmed:articleTitle |
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
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pubmed:affiliation |
Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-1951, USA. harold.mastalerz@bms.com
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pubmed:publicationType |
Journal Article
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