Synthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives.

Sinreih, Masa; Jójárt, Rebeka; Kele, Zoltán; Büdefeld, Tomaz; Paragi, Gábor; Mernyák, Erzsébet; Rizner, Tea Lanisnik

Sinreih, Masa; Jójárt, Rebeka; Kele, Zoltán; Büdefeld, Tomaz; Paragi, Gábor; Mernyák, Erzsébet; Rizner, Tea Lanisnik.

Afiliação

Sinreih M; Faculty of Medicine, Institute of Biochemistry and Molecular Genetics, University of Ljubljana, Ljubljana, Slovenia.
Jójárt R; Department of Organic Chemistry, University of Szeged, Szeged, Hungary.
Kele Z; Department of Medicinal Chemistry, University of Szeged, Szeged, Hungary.
Büdefeld T; Faculty of Medicine, Institute of Biochemistry and Molecular Genetics, University of Ljubljana, Ljubljana, Slovenia.
Paragi G; MTA-SZTE Biomimetic Systems Research Group, University of Szeged, Szeged, Hungary.
Mernyák E; Institute of Physics, University of Pécs, Pécs, Hungary.
Rizner TL; Department of Organic Chemistry, University of Szeged, Szeged, Hungary.

J Enzyme Inhib Med Chem ; 36(1): 1500-1508, 2021 Dec.

Article em En | MEDLINE | ID: mdl-34227437

Assuntos

20-Hidroxiesteroide Desidrogenases/antagonistas & inibidores; Inibidores Enzimáticos/farmacologia; Estrona/farmacologia; 20-Hidroxiesteroide Desidrogenases/metabolismo; Relação Dose-Resposta a Droga; Inibidores Enzimáticos/síntese química; Inibidores Enzimáticos/química; Estrona/análogos & derivados; Estrona/química; Humanos; Modelos Moleculares; Estrutura Molecular; Relação Estrutura-Atividade

Palavras-chave

Aldo-keto reductase; halogenated oestrone derivatives; inhibition; structureactivity relationships

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Estrona / 20-Hidroxiesteroide Desidrogenases Limite: Humans Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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