TY - JOUR
T1 - Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor
T2 - 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines
AU - Li, Hong Yu
AU - Wang, Yan
AU - Yan, Lei
AU - Campbell, Robert M.
AU - Anderson, Bryan D.
AU - Wagner, Jill R.
AU - Yingling, Jonathan M.
PY - 2004/7/5
Y1 - 2004/7/5
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=2942559053&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=2942559053&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2004.04.065
DO - 10.1016/j.bmcl.2004.04.065
M3 - Article
C2 - 15177480
AN - SCOPUS:2942559053
SN - 0960-894X
VL - 14
SP - 3585
EP - 3588
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 13
ER -