Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC<sub>50</sub> for a proof-of-principle study.

Abdelsamie, Ahmed S; van Koppen, Chris J; Bey, Emmanuel; Salah, Mohamed; Börger, Carsten; Siebenbürger, Lorenz; Laschke, Matthias W; Menger, Michael D; Frotscher, Martin

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC₅₀ for a proof-of-principle study.

Abdelsamie, Ahmed S; van Koppen, Chris J; Bey, Emmanuel; Salah, Mohamed; Börger, Carsten; Siebenbürger, Lorenz; Laschke, Matthias W; Menger, Michael D; Frotscher, Martin.

Afiliación

Abdelsamie AS; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany; Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, 12622 Cairo, Egypt.
van Koppen CJ; ElexoPharm GmbH, Campus A12, D-66123 Saarbrücken, Germany.
Bey E; ElexoPharm GmbH, Campus A12, D-66123 Saarbrücken, Germany.
Salah M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.
Börger C; PharmBioTec GmbH, Science Park 1, D-66123 Saarbrücken, Germany.
Siebenbürger L; PharmBioTec GmbH, Science Park 1, D-66123 Saarbrücken, Germany.
Laschke MW; Institute for Clinical and Experimental Surgery, Saarland University, D-66421, Homburg/Saar, Germany.
Menger MD; Institute for Clinical and Experimental Surgery, Saarland University, D-66421, Homburg/Saar, Germany.
Frotscher M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany. Electronic address: m.frotscher@mx.uni-saarland.de.

Eur J Med Chem ; 127: 944-957, 2017 Feb 15.

Article en En | MEDLINE | ID: mdl-27852458

Asunto(s)

17-Hidroxiesteroide Deshidrogenasas/antagonistas & inhibidores; Diseño de Fármacos; Inhibidores Enzimáticos/síntesis química; Inhibidores Enzimáticos/farmacología; Estrógenos/metabolismo; 17-Hidroxiesteroide Deshidrogenasas/metabolismo; Actinas/metabolismo; Animales; Técnicas de Química Sintética; Inhibidores Enzimáticos/metabolismo; Inhibidores Enzimáticos/farmacocinética; Receptor alfa de Estrógeno/metabolismo; Receptor beta de Estrógeno/metabolismo; Estudios de Factibilidad; Femenino; Humanos; Concentración 50 Inhibidora; Ratas; Especificidad por Sustrato

Palabras clave

17ß-Hydroxysteroid dehydrogenase type 1; Enzyme inhibitor; Estrogen-dependent disease; Intracrinology; Steroidogenic enzymes

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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Diseño de Fármacos / Inhibidores Enzimáticos / Estrógenos / 17-Hidroxiesteroide Deshidrogenasas Límite: Animals / Female / Humans Idioma: En Revista: Eur J Med Chem Año: 2017 Tipo del documento: Article País de afiliación: Egipto

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