2. Academic Validation
  3. Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines

  • Bioorg Med Chem Lett. 2004 Jul 5;14(13):3585-8. doi: 10.1016/j.bmcl.2004.04.065.
Hong-yu Li 1,  Yan Wang,  Lei Yan,  Robert M Campbell,  Bryan D Anderson,  Jill R Wagner,  Jonathan M Yingling
Affiliations

Affiliation

  • 1 Discovery Chemistry Research, Lilly Research Laboratory, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. [email protected]
PMID: 15177480 DOI: 10.1016/j.bmcl.2004.04.065
Abstract

A novel series of 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines was synthesized and their TbetaR-1 inhibitory, p38 MAPK inhibitory, and TbetaR-1-dependent cellular activity were evaluated. Compound 5a was found to be a highly potent in the enzyme assay and TbetaR-1-dependent cellular assays. In addition, dimer (4g), with a urea linker, shows a similar enzyme and cellular activity despite a bulky substitution.

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