کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1254701 | 971387 | 2014 | 6 صفحه PDF | دانلود رایگان |
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 abolished the four kinases inhibitory potency of compounds 2 and 3, but surprisingly, resulted in good activation effects on FGFR-1. Compounds 3d and 3g showed double-digit, nanomolar, selective activation effects on FGFR-1, and could be classified as first-generation small molecular activators of FGFR-1 kinase.
A series of novel, cycloalkyl-modified pazopanib analogs were designed and synthesized. Compounds 3d and 3g showed double-digit, nanomolar selective activation effects on FGFR-1, and could be classified as first-generation small molecular activators of FGFR-1 kinase.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 25, Issue 7, July 2014, Pages 989–994