Bioorganic and Medicinal Chemistry Letters p. 6788 - 6792 (2009)
Update date:2022-08-04
Topics: Molecular docking Enzyme inhibition Inhibitor Derivative Selectivity Testing Structure-Activity Relationship (SAR) In vitro assay Kinase assay Benzimidazole IC50 (Half-Maximal Inhibitory Concentration) Pharmacophore Modeling
Cole, Andrew G.
Bohnstedt, Adolph C.
Paradkar, Vidyadhar
Kingsbury, Celia
Quintero, Jorge G.
Park, Haengsoon
Lu, Yingchun
You, Ming
Neagu, Irina
Diller, David J.
Letourneau, Jeffrey J.
Shao, Yuefei
James, Ray A.
Riviello, Christopher M.
Ho, Koc-Kan
Lin, Tsung H.
Wang, Bojing
Appell, Kenneth C.
Sills, Matthew
Quadros, Elizabeth
Kimble, Earl F.
Ohlmeyer, Michael H.J.
Webb, Maria L.
A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-γ (INF-γ) production.
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Doi:10.1021/jm980170a
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