Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors

  • J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k.
Savithri Ramurthy  1 ,  Sharadha Subramanian ,  Mina Aikawa ,  Payman Amiri ,  Abran Costales ,  Jeff Dove ,  Susan Fong ,  Johanna M Jansen ,  Barry Levine ,  Sylvia Ma ,  Christopher M McBride ,  Jonah Michaelian ,  Teresa Pick ,  Daniel J Poon ,  Sandhya Girish ,  Cynthia M Shafer ,  Darrin Stuart ,  Leonard Sung ,  Paul A Renhowe
Affiliations
  • 1. Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, California 94608, USA. [email protected]
PMID: 18942827 DOI: 10.1021/jm801050k
Abstract

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.