1239411-93-8Relevant articles and documents
Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKβ inhibitors
Crombie, Aimee L.,Sum, Fuk-Wah,Powell, Dennis W.,Hopper, Darrin W.,Torres, Nancy,Berger, Dan M.,Zhang, Yixian,Gavriil, Maria,Sadler, Tammy M.,Arndt, Kim
scheme or table, p. 3821 - 3825 (2010/08/20)
A series of tricyclic anilinopyrimidines were synthesized and evaluated as IKKβ 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.
