Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Sheppeck, James E; Gilmore, John L; Yang, Anle; Chen, Xiao-Tao; Xue, Chu-Biao; Roderick, John; Liu, Rui-Qin; Covington, Maryanne B; Decicco, Carl P; Duan, James J-W

Sheppeck, James E; Gilmore, John L; Yang, Anle; Chen, Xiao-Tao; Xue, Chu-Biao; Roderick, John; Liu, Rui-Qin; Covington, Maryanne B; Decicco, Carl P; Duan, James J-W.

Afiliação

Sheppeck JE; Bristol-Myers Squibb Pharmaceutical Research Institute, Discovery Chemistry, PO Box 4000, Princeton, NJ 08543-4000, USA. jim.sheppeck@bms.com

Bioorg Med Chem Lett ; 17(5): 1413-7, 2007 Mar 01.

Article em En | MEDLINE | ID: mdl-17188863

ABSTRACT

ABSTRACT

A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. 5-Mono- and di-substituted hydantoins exhibited activity with IC50 values of 11-60 nM against porcine TACE in vitro and excellent selectivity against other MMPs.

Assuntos

Proteínas ADAM/antagonistas & inibidores; Hidantoínas/síntese química; Hidantoínas/farmacologia; Proteína ADAM17; Animais; Desenho de Fármacos; Concentração Inibidora 50; Relação Estrutura-Atividade; Especificidade por Substrato; Suínos

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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas ADAM / Hidantoínas Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Ano de publicação: 2007 Tipo de documento: Article

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