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.

Afiliación

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 en 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.

Asunto(s)

Proteínas ADAM/antagonistas & inhibidores; Hidantoínas/síntesis química; Hidantoínas/farmacología; Proteína ADAM17; Animales; Diseño de Fármacos; Concentración 50 Inhibidora; Relación Estructura-Actividad; Especificidad por Sustrato; Porcinos

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Base de datos: MEDLINE Asunto principal: Proteínas ADAM / Hidantoínas Tipo de estudio: Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article

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