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Discovery of Benzofuran Derivatives that Collaborate with Insulin-Like Growth Factor 1 (IGF-1) to Promote Neuroprotection

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posted on 09.05.2016, 20:30 by Takeshi Wakabayashi, Norihito Tokunaga, Kazuyuki Tokumaru, Taiichi Ohra, Nobuyuki Koyama, Satoru Hayashi, Ryuji Yamada, Mikio Shirasaki, Yoshitaka Inui, Tetsuya Tsukamoto
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.