Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives

H Hisamichi, R Naito, A Toyoshima, N Kawano…

Index: Hisamichi, Hiroyuki; Naito, Ryo; Toyoshima, Akira; Kawano, Noriyuki; Ichikawa, Atsushi; Orita, Akiko; Orita, Masaya; Hamada, Noritaka; Takeuchi, Makoto; Ohta, Mitsuaki; Tsukamoto, Shin-Ichi Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 16 p. 4936 - 4951

Full Text: HTML

Citation Number: 55

Abstract

Spleen tyrosine kinase (Syk) is a non-receptor-type tyrosine kinase which mediates diverse responses in haematopoietic cells. Therefore, Syk is an attractive therapeutic target, and in a study of Syk inhibitors as potentially new therapeutic agents, we discovered the 4- anilinopyrimidine-5-carboxamides. Enzyme screening indicated that an aminoethylamino moiety at the 2-position of the pyrimidine ring was important for Syk inhibitory activity, and ...