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)- …

…, Y Wang, L Yan, RM Campbell, BD Anderson…

Index: Li, Hong-Yu; Wang, Yan; Yan, Lei; Campbell, Robert M.; Anderson, Bryan D.; Wagner, Jill R.; Yingling, Jonathan M. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 13 p. 3585 - 3588

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Citation Number: 21

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 TβR-1 inhibitory, p38 MAPK inhibitory, and TβR-1- dependent cellular activity were evaluated. Compound 5a was found to be a highly potent in the enzyme assay and TβR-1-dependent cellular assays. In addition, dimer (4g), with a urea linker, shows a similar enzyme and cellular activity despite a bulky substitution.