SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 24, 2012, Pages 7653-7658

  Forsyth, Timothy ^a   Kearney, Patrick C ^a   Kim, Byung Gyu ^a   Johnson, Henry W B ^a   Aay, Naing ^a   Arcalas, Arlyn ^a   Brown, David S ^a   Chan, Vicky ^a   Chen, Jeff ^a   Du, Hongwang ^a   Epshteyn, Sergey ^a   Galan, Adam A ^a   Huynh, Tai P ^a   Ibrahim, Mohamed A ^a   Kane, Brian ^a   Koltun, Elena S ^a   Mann, Grace ^a   Meyr, Lisa E ^a   Lee, Matthew S ^a   Lewis, Gary L ^a   Noguchi, Robin T ^a   Pack, Michael ^a   Ridgway, Brian H ^a   Shi, Xian ^a   Takeuchi, Craig S ^a   Zu, Peiwen ^a   Leahy, James W ^a   Nuss, John M ^a   Aoyama, Ron ^a   Engst, Stefan ^a   Gendreau, Steven B ^a   Kassees, Robert ^a   Li, Jia ^a   Lin, Shwu Hwa ^a   Martini, Jean Francois ^a   Stout, Thomas ^a   Tong, Philip ^a   Woolfrey, John ^a   Zhang, Wentao ^a   Yu, Peiwen ^a   more..

^a EXELIXIS INC   (United States)

Author keywords

4 Aryl 2 aminoalkylpyrimidine; JAK1; JAK2; JAK3

Indexed keywords

ANTINEOPLASTIC AGENT; JANUS KINASE 2 INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG; XL 019;

ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; HIGH THROUGHPUT SCREENING; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; HAPLORHINI; HIGH-THROUGHPUT SCREENING ASSAYS; JANUS KINASE 2; MICE; MICE, NUDE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; PROTEIN KINASE INHIBITORS; PYRIMIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84870249023     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.10.007     Document Type: Article

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