2. Academic Validation
  3. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors

Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors

  • Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4. doi: 10.1016/j.bmcl.2004.07.061.
Masahiro Tanaka 1,  Shoichi Sagawa,  Jun-ichi Hoshi,  Fumito Shimoma,  Isamu Matsuda,  Kenji Sakoda,  Tomohiko Sasase,  Masanori Shindo,  Takashi Inaba
Affiliations

Affiliation

  • 1 Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
PMID: 15380221 DOI: 10.1016/j.bmcl.2004.07.061
Abstract

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).

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