Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors. Issue 10 (15th May 2017)

• Record Type: Journal Article
• Authors: Matsumaru, Takanori; Inai, Makoto; Ishigami, Kana; Iwamatsu, Toshiki; Maita, Hiroshi; Otsuguro, Satoko; Nomura, Takao; Matsuda, Akira; Ichikawa, Satoshi; Sakaitani, Masahiro; Shuto, Satoshi; Maenaka, Katsumi; Kan, Toshiyuki
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 10(2017)
• Page Start: 2144
• Page End: 2147
• Publication Date: 2017-05-15
• Subjects: BAY 61-3606 -- Imidazo[1, 2-c]pyrimidine -- Gck -- Indole -- Kinase inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.055
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.