Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.

Krämer, Andreas; Kurz, Christian Georg; Berger, Benedict-Tilman; Celik, Ibrahim Ethem; Tjaden, Amelie; Greco, Francesco Aleksy; Knapp, Stefan; Hanke, Thomas

Krämer, Andreas; Kurz, Christian Georg; Berger, Benedict-Tilman; Celik, Ibrahim Ethem; Tjaden, Amelie; Greco, Francesco Aleksy; Knapp, Stefan; Hanke, Thomas.

Afiliação

Krämer A; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany; Frankfurt Cancer Institute (FCI), Paul-Ehrli
Kurz CG; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany.
Berger BT; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany.
Celik IE; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany.
Tjaden A; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany.
Greco FA; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany.
Knapp S; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany; German Translational Cancer Network (DKTK) S
Hanke T; Institute of Pharmaceutical Chemistry, Max-von-Laue-Straße 9, Goethe University Frankfurt, 60438, Frankfurt, Germany; Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences (BMLS), Max-von-Laue-Straße 15, 60438, Frankfurt, Germany. Electronic address: hanke@pharmchem.uni-fran

Eur J Med Chem ; 208: 112770, 2020 Dec 15.

Article em En | MEDLINE | ID: mdl-32883634

Assuntos

Inibidores de Proteínas Quinases/farmacologia; Pirazóis/farmacologia; Pirimidinas/farmacologia; Sítios de Ligação; Caseína Quinase II/antagonistas & inibidores; Caseína Quinase II/química; Caseína Quinase II/metabolismo; Cristalografia por Raios X; Células HEK293; Humanos; Estrutura Molecular; Ligação Proteica; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/metabolismo; Pirazóis/síntese química; Pirazóis/metabolismo; Pirimidinas/síntese química; Pirimidinas/metabolismo; Relação Estrutura-Atividade

Palavras-chave

Antiproliferative activity; Casein kinase 2 inhibitor; Macrocyclic kinase inhibitor; NanoBRET; Pyrazolo[1,5-a]pyrimidines; X-ray

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirazóis / Pirimidinas / Inibidores de Proteínas Quinases Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2020 Tipo de documento: Article

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