| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10593163 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
The imidazoquinoline derivative 1 was found as a novel mPGES-1 inhibitor. Optimization of 1 led to the identification of the 2-chlorophenyl group at the C(2)-position and the quinolone structure at the C(4)-position. Compound 33, the most potent synthesized compound, showed excellent mPGES-1 inhibition (IC50Â =Â 9.1Â nM) with high selectivity (>1000-fold) over both COX-1 and COX-2.
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Authors
Tomoya Shiro, Hirotada Takahashi, Keisuke Kakiguchi, Yoshifumi Inoue, Keiki Masuda, Hidetaka Nagata, Masanori Tobe,