Discovery and synthesis of N2,N4-substitued-cycloalkyl[d]pyrimidine 2,4-diamine analogs： The first examples of small-molecular FGFR-1 activator

• Published in: Chinese chemical letters Vol. 25; no. 7; pp. 989 - 994
• Main Authors: Li, Bao-Li, Xiao, Fang, Lu, Wen-Chao, Sun, Yu-Yun, Zhu, Jin, Li, Jian
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.07.2014
• Subjects: Activator; Chemical probe; Cycloalkyl[d]pyrimidine derivatives; FGFR-1; 个例; 合成; 嘧啶; 小分子; 激活作用; 环烷基; 类似物; Cycloalkyl[d]pyrimidine derivatives; Chemical probe; Activator; FGFR-1

A series of novel, cycloalkyl-modified pazopanib analogs 2 and 3 were designed and synthesized. Their kinase modulatory effects on FGFR-1, VEGFR-2, PDGFR-β and c-KIT were evaluated by the caliper mobility shift assay. Introduction of cycloalkyl into the pyrimidine linker of pazopanib almost abolishe...