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Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors

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Title: Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors
Authors: Matsumaru, Takanori Browse this author
Inai, Makoto Browse this author
Ishigami, Kana Browse this author
Iwamatsu, Toshiki Browse this author
Maita, Hiroshi Browse this author →KAKEN DB
Otsuguro, Satoko Browse this author
Nomura, Takao Browse this author
Matsuda, Akira Browse this author →KAKEN DB
Ichikawa, Satoshi Browse this author →KAKEN DB
Sakaitani, Masahiro Browse this author
Shuto, Satoshi Browse this author →KAKEN DB
Maenaka, Katsumi Browse this author →KAKEN DB
Kan, Toshiyuki Browse this author
Keywords: BAY 61-3606
Imidazo[1,2-c]pyrimidine
Gck
Indole
Kinase inhibitor
Issue Date: 15-May-2017
Publisher: Elsevier
Journal Title: Bioorganic & medicinal chemistry letters
Volume: 27
Issue: 10
Start Page: 2144
End Page: 2147
Publisher DOI: 10.1016/j.bmcl.2017.03.055
Abstract: We accomplished divergent synthesis of potent kinase inhibitor BAY 61-3606 (1) and 27 derivatives via conjugation of imidazo[1,2-c]pyrimidine and indole ring compounds with aromatic (including pyridine) derivatives by means of palladium-catalyzed cross-coupling reaction. Spleen tyrosine kinase (Syk) and germinal center kinase (Gck, MAP4K2) inhibition assays showed that some of the synthesized compounds were selective Gck inhibitors. (C) 2017 Elsevier Ltd. All rights reserved.
Rights: ©2017. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
http://creativecommons.org/licenses/by-nc-nd/4.0/
Type: article (author version)
URI: http://hdl.handle.net/2115/74002
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 松丸 尊紀

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