Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17ß-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.

Abdelsamie, Ahmed S; Salah, Mohamed; Siebenbürger, Lorenz; Hamed, Mostafa M; Börger, Carsten; van Koppen, Chris J; Frotscher, Martin; Hartmann, Rolf W

Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17ß-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.

Abdelsamie, Ahmed S; Salah, Mohamed; Siebenbürger, Lorenz; Hamed, Mostafa M; Börger, Carsten; van Koppen, Chris J; Frotscher, Martin; Hartmann, Rolf W.

Afiliação

Abdelsamie AS; Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI), Department of Drug Design and Optimization, Campus Building E8.1, 66123, Saarbrücken, Germany; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken
Salah M; Department of Pharmaceutical and Medicinal Chemistry, Saarland University, 66123, Saarbrücken, Germany.
Siebenbürger L; PharmBioTec GmbH, Science Park 1, 66123, Saarbrücken, Germany.
Hamed MM; Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI), Department of Drug Design and Optimization, Campus Building E8.1, 66123, Saarbrücken, Germany; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken
Börger C; PharmBioTec GmbH, Science Park 1, 66123, Saarbrücken, Germany.
van Koppen CJ; Department of Pharmaceutical and Medicinal Chemistry, Saarland University, 66123, Saarbrücken, Germany; ElexoPharm GmbH, Im Stadtwald, Building A1.2, 66123, Saarbrücken, Germany.
Frotscher M; Department of Pharmaceutical and Medicinal Chemistry, Saarland University, 66123, Saarbrücken, Germany.
Hartmann RW; Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI), Department of Drug Design and Optimization, Campus Building E8.1, 66123, Saarbrücken, Germany; Department of Pharmaceutical and Medicinal Chemistry, Saarland University, 66123, Saarbrücke

Eur J Med Chem ; 178: 93-107, 2019 Sep 15.

Article em En | MEDLINE | ID: mdl-31176098

Assuntos

17-Hidroxiesteroide Desidrogenases/antagonistas & inibidores; Inibidores Enzimáticos/farmacocinética; Estradiol Desidrogenases/antagonistas & inibidores; Fenóis/farmacocinética; Tiofenos/farmacocinética; Animais; Sítios de Ligação; Desenho de Fármacos; Estabilidade de Medicamentos; Inibidores Enzimáticos/síntese química; Inibidores Enzimáticos/química; Inibidores Enzimáticos/metabolismo; Estradiol Desidrogenases/química; Estradiol Desidrogenases/metabolismo; Células HEK293; Humanos; Camundongos; Microssomos Hepáticos/metabolismo; Simulação de Acoplamento Molecular; Estrutura Molecular; Fenóis/síntese química; Fenóis/química; Fenóis/metabolismo; Ligação Proteica; Solubilidade; Relação Estrutura-Atividade; Tiofenos/síntese química; Tiofenos/química; Tiofenos/metabolismo

Palavras-chave

17ß-hydroxysteroid dehydrogenase; Bicyclic substituted hydroxyphenylmethanones class; Endometriosis; Estradiol; Estrone; Osteoporosis

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenóis / Tiofenos / Inibidores Enzimáticos / Estradiol Desidrogenases / 17-Hidroxiesteroide Desidrogenases Limite: Animals / Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2019 Tipo de documento: Article

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