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Tetracyclic sulfones as potent gamma-secretase inhibitors: synthesis and structure-activity relationship studies.
Sasikumar, T K; Burnett, Duane A; Asberom, Theodros; Wu, Wen-Lian; Bennett, Chad; Cole, David; Xu, Ruo; Greenlee, William J; Clader, John; Zhang, Lili; Hyde, Lynn.
Afiliação
  • Sasikumar TK; Merck Research Laboratories, Kenilworth, NJ 07033, USA. sasikumartk@yahoo.com
Bioorg Med Chem Lett ; 20(12): 3645-8, 2010 Jun 15.
Article em En | MEDLINE | ID: mdl-20471254
Complex tetracyclic sulfones were designed as gamma-secretase inhibitors and a stereoselective synthesis was achieved. Gamma-secretase activity was seen predominately in the (-) enantiomeric series. Compounds such as 2a and 2b showed remarkable in vitro and in vivo potency.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Sulfonas / Secretases da Proteína Precursora do Amiloide Limite: Animals / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Sulfonas / Secretases da Proteína Precursora do Amiloide Limite: Animals / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article