Autor: |
Tanaka M; Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan., Sagawa S, Hoshi J, Shimoma F, Matsuda I, Sakoda K, Sasase T, Shindo M, Inaba T |
Jazyk: |
angličtina |
Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Oct 18; Vol. 14 (20), pp. 5171-4. |
DOI: |
10.1016/j.bmcl.2004.07.061 |
Abstrakt: |
We report herein synthesis of PKCbeta-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide. Several compounds of this series exhibited IC50's as low as 50 nM against human PKCbeta2. One of the most potent compounds, 6l, inhibited PKCbeta1 and PKCbeta2 with IC50 of 21 and 5 nM, respectively, and exhibited selectivity of more than 60-fold in favor of PKCbeta2 relative to other PKC isozymes (PKCalpha, PKCgamma, and PKCepsilon). |
Databáze: |
MEDLINE |
Externí odkaz: |
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