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Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4] triazoles as inhibitors of transforming growth factor β1 type 1 receptor

Title
Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4] triazoles as inhibitors of transforming growth factor β1 type 1 receptor
Authors
Kim D.-K.Kim J.Park H.-J.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2004
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
Bioorganic and Medicinal Chemistry vol. 12, no. 9, pp. 2013 - 2020
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
A series of 2-pyridinyl-[1,2,4]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 12b showed significant ALK5 inhibition (SBE-Luciferase, 73%; p3TP-Luciferase, 85%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-Luciferase, 79%; p3TP-Luciferase, 88%), but weak p38α MAP kinase inhibition (4%) at a concentration of 10μM that is much lower than that of SB-431542 (54%). The binding mode of 12b generated by flexible docking studies revealed that the structure of 12b is a good fit into the (NPC-30345)-binding cavity of ALK5. © 2004 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2004.03.004
Appears in Collections:
약학대학 > 약학과 > Journal papers
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