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2005 Indole derivatives R 0140 Synthesis of Anilino-monoindolylmaleimides as Potent and Selective PKCβ Inhib- itors. — A new class of anilino-monoindolylmaleimides [cf. (V), (X)] are prepared and evaluated for their PKCβ2 inhibitory activity and selectivity. Compounds (Xa) and (Xe) show good activity for PCKβ2 with remarkable selectivity over other calcium-de- pendent isozymes (PKCα and PKCγ) and the calcium-independent isozyme (PKCε). — (TANAKA, M.; SAGAWA, S.; HOSHI, J.-I.; SHIMONA, F.; MATSUDA, I.; SAKODA, K.; SASASE, T.; SHINDO, M.; INABA*, T.; Bioorg. Med. Chem. Lett. 14 (2004) 20, 5171-5174; Cent. Pharm. Res. Inst., Japan Tobacco Inc., Takatsuki, Osaka 569, Japan; Eng.) — M. Bohle 05- 104

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Page 1: Synthesis of Anilino-monoindolylmaleimides as Potent and Selective PKCβ Inhibitors

2005

Indole derivativesR 0140 Synthesis of Anilino-monoindolylmaleimides as Potent and Selective PKCβ Inhib-

itors. — A new class of anilino-monoindolylmaleimides [cf. (V), (X)] are prepared and evaluated for their PKCβ2 inhibitory activity and selectivity. Compounds (Xa) and (Xe) show good activity for PCKβ2 with remarkable selectivity over other calcium-de-pendent isozymes (PKCα and PKCγ) and the calcium-independent isozyme (PKCε). — (TANAKA, M.; SAGAWA, S.; HOSHI, J.-I.; SHIMONA, F.; MATSUDA, I.; SAKODA, K.; SASASE, T.; SHINDO, M.; INABA*, T.; Bioorg. Med. Chem. Lett. 14 (2004) 20, 5171-5174; Cent. Pharm. Res. Inst., Japan Tobacco Inc., Takatsuki, Osaka 569, Japan; Eng.) — M. Bohle

05- 104

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