| 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)
|
