Synthesis and biological evaluation on novel analogs of 9-methylstreptimidone, an inhibitor of NF-kappaB.

Ishikawa, Yuichi; Tachibana, Miyuki; Matsui, Chino; Obata, Rika; Umezawa, Kazuo; Nishiyama, Shigeru

Ishikawa, Yuichi; Tachibana, Miyuki; Matsui, Chino; Obata, Rika; Umezawa, Kazuo; Nishiyama, Shigeru.

Afiliação

Ishikawa Y; Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.

Bioorg Med Chem Lett ; 19(6): 1726-8, 2009 Mar 15.

Article em En | MEDLINE | ID: mdl-19231181

ABSTRACT

ABSTRACT

Synthesis of 9-methylstreptimidone analogs and their inhibitory activities against NF-kappaB (nuclear factor-kappaB) are reported. Among several active derivatives synthesized in this study, 8 with a relatively simple structure, exhibited inhibitory activity against LPS-induced NO production comparable to that of 9-methylstreptimidone.

Assuntos

Lipopolissacarídeos/química; NF-kappa B/antagonistas & inibidores; Neoplasias/tratamento farmacológico; Óxido Nítrico/química; Piperidonas/síntese química; Piperidonas/farmacologia; Animais; Antioxidantes/metabolismo; Linhagem Celular Tumoral; Química Farmacêutica/métodos; Desenho de Fármacos; Humanos; Concentração Inibidora 50; Células Jurkat; Camundongos; Modelos Químicos; NF-kappa B/química

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidonas / Lipopolissacarídeos / NF-kappa B / Neoplasias / Óxido Nítrico Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2009 Tipo de documento: Article

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