5VGO

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

Wang, X., Barbosa, J., Blomgren, P., Bremer, M.C., Chen, J., Crawford, J.J., Deng, W., Dong, L., Eigenbrot, C., Gallion, S., Hau, J., Hu, H., Johnson, A.R., Katewa, A., Kropf, J.E., Lee, S.H., Liu, L., Lubach, J.W., Macaluso, J., Maciejewski, P., Mitchell, S.A., Ortwine, D.F., DiPaolo, J., Reif, K., Scheerens, H., Schmitt, A., Wong, H., Xiong, J.M., Xu, J., Zhao, Z., Zhou, F., Currie, K.S., Young, W.B.

(2017) ACS Med Chem Lett 8: 608-613

• PubMed: 28626519 Search on PubMedSearch on PubMed Central
• DOI: https://doi.org/10.1021/acsmedchemlett.7b00103
• Primary Citation of Related Structures:  
  5VGO


• PubMed Abstract: 
  

  In our continued effort to discover and develop best-in-class Bruton's tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds that improved upon the druglike properties of our previous chemical matter. Compounds exemplified by G-744 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.

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Organizational Affiliation: 

Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.