Document Report Card
Basic Information
ID: ALA1137681
Journal: Eur J Med Chem
Title: Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.
Authors: Peifer C, Bühler S, Hauser D, Kinkel K, Totzke F, Schächtele C, Laufer S.
Abstract: In this study we report on the design, synthesis and biological characterization of novel N(9) or N(7) arylethanone-substituted 6-aminopurines and 6-methoxypurines, respectively, as EGF-R and VEGF-R inhibitors. The compounds were initially profiled in a panel of 24 cancer-relevant protein kinases. Dependent on the regio-substitution of the purine core we found inhibition activity for EGF-R and VEGF-R with IC(50) values in the microM range. The two novel N(9)/N(7) 2-(6-amino-purine)-1-(1H-indole-3-yl)ethanone derivatives were characterized in an enhanced panel of 78 kinases showing the N(9) derivative to also inhibit MNK1 and IRR while the N(7) isomer was found to be specific for VEGF-R2.
CiteXplore: 18524423