Efficient synthesis of novel disubstituted pyrido[3,4-b]pyrazines for the design of protein kinase inhibitors

作者：Antoine Maud; Schuster Tilmann; Seipelt Irene; Aicher Babette; Teifel Michael; Guenther Eckhard; Gerlach Matthias; Marchand Pascal^*

来源：Medchemcomm, 2016, 7(2): 224-229.

DOI：10.1039/c5md00424a

A novel family of disubstituted pyrido [3,4-b] pyrazine-based compounds was discovered as valuable series for the design of promising protein kinase inhibitors. SAR study allowed the identification of 4-(piperidin-1-yl) aniline moiety as pharmacophoric group, in C-5 or C-8 positions of the pyrido [3,4-b] pyrazine ring, for binding to the selected therapeutic targets. Several analogues were active at low micromomolar IC50 values against a panel of seven cancer-related protein kinases providing an excellent starting point for further drug discovery optimization.

• 出版日期2016