@article{f0383e918e9146998f0ff13681de3436,
title = "Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors",
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.",
keywords = "BAY 61-3606, Gck, Imidazo[1,2-c]pyrimidine, Indole, Kinase inhibitor",
author = "Takanori Matsumaru and Makoto Inai and Kana Ishigami and Toshiki Iwamatsu and Hiroshi Maita and Satoko Otsuguro and Takao Nomura and Akira Matsuda and Satoshi Ichikawa and Masahiro Sakaitani and Satoshi Shuto and Katsumi Maenaka and Toshiyuki Kan",
note = "Funding Information: This research is (partially) supported by the Platform Project for Supporting in Drug Discovery and Life Science Research (Platform for Drug Discovery, Informatics, and Structural Life Science) from the Ministry of Education, Culture, Sports, Science (MEXT) and Japan Agency for Medical Research and development (AMED).",
year = "2017",
doi = "10.1016/j.bmcl.2017.03.055",
language = "English",
volume = "27",
pages = "2144--2147",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "10",
}