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Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Stevens, Kirk L; Alligood, Krystal J; Alberti, Jennifer G Badiang; Caferro, Thomas R; Chamberlain, Stanley D; Dickerson, Scott H; Dickson, Hamilton D; Emerson, Holly K; Griffin, Robert J; Hubbard, Robert D; Keith, Barry R; Mullin, Robert J; Petrov, Kimberly G; Gerding, Roseanne M; Reno, Michael J; Rheault, Tara R; Rusnak, David W; Sammond, Douglas M; Smith, Stephon C; Uehling, David E; Waterson, Alex G; Wood, Edgar R.
Afiliação
  • Stevens KL; Department of Oncology Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. Kirk.L.Stevens@GSK.com
Bioorg Med Chem Lett ; 19(1): 21-6, 2009 Jan 01.
Article em En | MEDLINE | ID: mdl-19028424
ABSTRACT
A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range of effects on enzyme and cellular potency. In addition, the impact of the absolute stereochemical configuration on cellular potency and oral mouse pharmacokinetics is described.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Pirrolidinas / Receptor ErbB-2 / Receptores ErbB / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2009 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Pirrolidinas / Receptor ErbB-2 / Receptores ErbB / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2009 Tipo de documento: Article