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Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
- Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
- Kim D.-K.; Kim J.; Park H.-J.
- Ewha Authors
- SCOPUS Author ID
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- Journal Title
- Bioorganic and Medicinal Chemistry Letters
- Bioorganic and Medicinal Chemistry Letters vol. 14, no. 10, pp. 2401 - 2405
- SCI; SCIE; SCOPUS
- Document Type
- 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%). © 2004 Elsevier Ltd. All rights reserved.
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