2. Academic Validation
  3. 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3245-50. doi: 10.1016/j.bmcl.2004.03.090.
Han-Cheng Zhang 1,  Hong Ye,  Bruce R Conway,  Claudia K Derian,  Michael F Addo,  Gee-Hong Kuo,  Leonard R Hecker,  Diane R Croll,  Jian Li,  Lori Westover,  Jun Z Xu,  Richard Look,  Keith T Demarest,  Patricia Andrade-Gordon,  Bruce P Damiano,  Bruce E Maryanoff
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477-0776, USA. hzhang@prdus.jnj.com
PMID: 15149684 DOI: 10.1016/j.bmcl.2004.03.090
Abstract

A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was synthesized and evaluated for activity against GSK-3beta and selectivity versus PKC-betaII, as well as a broad panel of protein kinases. Compounds 14 and 17c potently inhibited GSK-3beta (IC(50)=7 and 26 nM, respectively) and exhibited excellent selectivity over PKC-betaII (325 and >385-fold, respectively). Compound 17c was also highly selective against 68 Other protein kinases. In a cell-based functional assay, both 14 and 17c effectively increased glycogen synthase activity by inhibiting GSK-3beta.

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