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Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor.
Collin, Marie-Pierre; Lobell, Mario; Hübsch, Walter; Brohm, Dirk; Schirok, Hartmut; Jautelat, Rolf; Lustig, Klemens; Bömer, Ulf; Vöhringer, Verena; Héroult, Mélanie; Grünewald, Sylvia; Hess-Stumpp, Holger.
Afiliação
  • Collin MP; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Lobell M; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Hübsch W; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Brohm D; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Schirok H; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Jautelat R; Department of Medicinal Chemistry, Drug Discovery, Bayer AG, Postfach 101709, 42096, Wuppertal, Germany.
  • Lustig K; Research Pharmacokinetics Group, Drug Discovery, Bayer AG, Germany.
  • Bömer U; Lead Discovery, Drug Discovery, Bayer AG, Germany.
  • Vöhringer V; Therapeutic Research Group, Oncology, Drug Discovery, Bayer AG, Germany.
  • Héroult M; Therapeutic Research Group, Oncology, Drug Discovery, Bayer AG, Germany.
  • Grünewald S; Therapeutic Research Group, Oncology, Drug Discovery, Bayer AG, Germany.
  • Hess-Stumpp H; Therapeutic Research Group, Oncology, Drug Discovery, Bayer AG, Germany.
ChemMedChem ; 13(5): 437-445, 2018 03 06.
Article em En | MEDLINE | ID: mdl-29451369
ABSTRACT
Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1-4) for oral application currently being investigated in phase 1 clinical trials for the treatment of cancer. In this publication, we report its discovery by de novo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Pirróis / Tiofenos / Inibidores de Proteínas Quinases / Receptor Tipo 1 de Fator de Crescimento de Fibroblastos / Bibliotecas de Moléculas Pequenas / Descoberta de Drogas Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Pirróis / Tiofenos / Inibidores de Proteínas Quinases / Receptor Tipo 1 de Fator de Crescimento de Fibroblastos / Bibliotecas de Moléculas Pequenas / Descoberta de Drogas Idioma: En Ano de publicação: 2018 Tipo de documento: Article