Bioorganic and Medicinal Chemistry Letters p. 3821 - 3825 (2010)
Update date:2022-08-05
Topics:
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
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.
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