TY - JOUR
T1 - Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
AU - Kim, Dae Kee
AU - Kim, Joonseop
AU - Park, Hyun Ju
PY - 2004/5/17
Y1 - 2004/5/17
N2 - A series of 2-pyridinyl-[1,2,3]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 inhibition (SBE-luciferase activity, 25%; p3TP-luciferase activity, 17%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38α MAP kinase inhibition (13%) at a concentration of 10μM that is much lower than that of SB-431542 (54%).
AB - A series of 2-pyridinyl-[1,2,3]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 inhibition (SBE-luciferase activity, 25%; p3TP-luciferase activity, 17%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38α MAP kinase inhibition (13%) at a concentration of 10μM that is much lower than that of SB-431542 (54%).
KW - 2-Pyridinyl-[1,2,3]triazoles
KW - ALK5
KW - Inhibitors
KW - TGF-β1 type 1 receptor
UR - https://www.scopus.com/pages/publications/1942534588
U2 - 10.1016/j.bmcl.2004.03.024
DO - 10.1016/j.bmcl.2004.03.024
M3 - Article
C2 - 15109621
AN - SCOPUS:1942534588
SN - 0960-894X
VL - 14
SP - 2401
EP - 2405
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 10
ER -
