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Discovery and structure-activity relationships of spiroindolines as novel inducers of oligodendrocyte progenitor cell differentiation.
Katayama, Katsushi; Arai, Yoshikazu; Murata, Kenji; Saito, Shoichi; Nagata, Tsutomu; Takashima, Kouhei; Yoshida, Ayako; Masumura, Makoto; Koda, Shuichi; Okada, Hiroyuki; Muto, Tsuyoshi.
Afiliação
  • Katayama K; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan. Electronic address: katayama.katsushi.ne@daiichisankyo.co.jp.
  • Arai Y; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Murata K; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Saito S; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Nagata T; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Takashima K; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Yoshida A; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Masumura M; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Koda S; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Okada H; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
  • Muto T; Asubio Pharma Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
Bioorg Med Chem ; 28(6): 115348, 2020 03 15.
Article em En | MEDLINE | ID: mdl-32046916
A novel series of spiroindoline derivatives was discovered for use as inducers of oligodendrocyte progenitor cell (OPC) differentiation, resulting from optimization of screening hit 1. Exploration of structure-activity relationships led to compound 18, which showed improved potency (rOPC EC50 = 0.0032 µM). Furthermore, oral administration of compound 18 significantly decreased clinical severity in an experimental autoimmune encephalomyelitis (EAE) model.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Encefalomielite Autoimune Experimental / Descoberta de Drogas / Células Precursoras de Oligodendrócitos / Indóis Limite: Animals Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Encefalomielite Autoimune Experimental / Descoberta de Drogas / Células Precursoras de Oligodendrócitos / Indóis Limite: Animals Idioma: En Ano de publicação: 2020 Tipo de documento: Article