title: Discovery of Benzofuran Derivatives that Collaborate with Insulin-Like Growth Factor 1 (IGF-1) to Promote Neuroprotection.
abstract: A series of benzofuran derivatives with neuroprotective activity in collaboration with IGF-1 was discovered using a newly developed cell-based assay involving primary neural cells prepared from rat hippocampal and cerebral cortical tissues. A structure-activity relationship study identified compound 8 as exhibiting potent activity and brain penetrability. An in vitro pharmacological study demonstrated that although IGF-1 and 8 individually exhibited the neuroprotective effect, the latter acted in collaboration with IGF-1 to enhance neuroprotective activity.
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Takeshi
authors.initials: T
authors.lastname: Wakabayashi
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Norihito
authors.initials: N
authors.lastname: Tokunaga
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Tokumaru
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Taiichi
authors.initials: T
authors.lastname: Ohra
authors.affiliation: Japan Oncology Business Unit, Takeda Pharmaceutical Company, Ltd. , 12-10, Nihonbashi 2-chome, Chuo-ku, Tokyo 103-8668, Japan.
authors.forename: Nobuyuki
authors.initials: N
authors.lastname: Koyama
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Satoru
authors.initials: S
authors.lastname: Hayashi
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Ryuji
authors.initials: R
authors.lastname: Yamada
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Mikio
authors.initials: M
authors.lastname: Shirasaki
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Yoshitaka
authors.initials: Y
authors.lastname: Inui
authors.affiliation: Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd. , 26-1 Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Tsukamoto
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D007334:Insulin-Like Growth Factor I / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D009474:Neurons / Q000187:drug effects*; D000066829:Neuroprotection / Q000187:drug effects; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D001572:Benzofurans; D018696:Neuroprotective Agents; D007334:Insulin-Like Growth Factor I; C105430:benzofuran