Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7

J Med Chem. 2006 Mar 23;49(6):2138-42. doi: 10.1021/jm058209g.

Hong-yu Li ¹, Yan Wang, Charles R Heap, Chi-Hsin R King, Sreenivasa R Mundla, Matthew Voss, David K Clawson, Lei Yan, Robert M Campbell, Bryan D Anderson, Jill R Wagner, Karen Britt, Ku X Lu, William T McMillen, Jonathan M Yingling

Affiliations

Affiliation

1 Discovery Chemistry Research and Technology, Lilly Research Laboratory, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. li_hong-yu@lilly.com

PMID: 16539403 DOI: 10.1021/jm058209g

Abstract

Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus TGF-beta RII and MLK-7 kinases. Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay.

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