Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKbeta inhibitors.
Basic Information
ID: ALA1155535
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKbeta inhibitors.
Authors: Crombie AL, Sum FW, Powell DW, Hopper DW, Torres N, Berger DM, Zhang Y, Gavriil M, Sadler TM, Arndt K.
Abstract: A series of tricyclic anilinopyrimidines were synthesized and evaluated as IKKbeta inhibitors. Several analogues, including tricyclic phenyl (10, 18a, 18c, 18d, and 18j) and thienyl (26 and 28) derivatives were shown to have good in vitro enzyme potency and excellent cellular activity. Pharmaceutical profiling of a select group of tricyclic compounds compared to the non-tricyclic analogues suggested that in some cases, the improved cellular activity may be due to increased clog P and permeability.
CiteXplore: 20471256
DOI: 10.1016/j.bmcl.2010.04.022
Patent ID: ┄