Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

Dae Kee Kim; Joonseop Kim; Hyun Ju Park

doi:10.1016/j.bmcl.2004.03.024

Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

Dae Kee Kim, Joonseop Kim, Hyun Ju Park

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

93 Scopus citations

Abstract

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%).

Original language	English
Pages (from-to)	2401-2405
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2004.03.024
State	Published - 17 May 2004

Bibliographical note

Funding Information:
This work was supported by a grant from KISTEP, Korea (M1-0310-43-0000).

Keywords

2-Pyridinyl-[1,2,3]triazoles
ALK5
Inhibitors
TGF-β1 type 1 receptor

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10.1016/j.bmcl.2004.03.024

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title = "Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor",

abstract = "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%).",

keywords = "2-Pyridinyl-[1,2,3]triazoles, ALK5, Inhibitors, TGF-β1 type 1 receptor",

author = "Kim, {Dae Kee} and Joonseop Kim and Park, {Hyun Ju}",

note = "Funding Information: This work was supported by a grant from KISTEP, Korea (M1-0310-43-0000).",

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doi = "10.1016/j.bmcl.2004.03.024",

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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

N1 - Funding Information: This work was supported by a grant from KISTEP, Korea (M1-0310-43-0000).

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

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JO - Bioorganic and Medicinal Chemistry Letters

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IS - 10

ER -

Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

Abstract

Bibliographical note

Keywords

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