Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 9, 2013, Pages 2522-2526

  Jaime Figueroa, Saul ^a   De Vicente, Javier ^a   Hermann, Johannes ^a   Jahangir, Alam ^b   Jin, Sue ^a   Kuglstatter, Andreas ^a,b   Lynch, Stephen M ^a   Menke, John ^a   Niu, Linghao ^a   Patel, Vaishali ^a   Shao, Ada ^b   Soth, Michael ^a   Vu, Minh Diem ^a   Yee, Calvin ^a  

^a HOFFMANN LA ROCHE INC   (United States)

^b ROCHE BIOSCIENCE   (United States)

Author keywords

JAK; JAK3; Janus kinase; Kinase inhibitors; Structure based drug design

Indexed keywords

5H PYRROLO[2,3 B]PYRAZINE 2 PHENYL ETHER DERIVATIVE; JANUS KINASE 1; JANUS KINASE 2; JANUS KINASE 3; JANUS KINASE 3 INHIBITOR; PYRAZINE DERIVATIVE; TOFACITINIB; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; ENZYME STRUCTURE; IC 50; PROTEIN DOMAIN; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CATALYTIC DOMAIN; DRUG EVALUATION, PRECLINICAL; JANUS KINASE 3; MOLECULAR DOCKING SIMULATION; PHENYL ETHERS; PROTEIN BINDING; PROTEIN ISOFORMS; PROTEIN KINASE INHIBITORS; PYRIDAZINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84876149586     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.03.015     Document Type: Article

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