Literature DB >> 15109621

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

Dae-Kee Kim1, Joonseop Kim, Hyun-Ju Park.   

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 5 microM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38 alpha MAP kinase inhibition (13%) at a concentration of 10 microM that is much lower than that of SB-431542 (54%).

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Year:  2004        PMID： 15109621     DOI： 10.1016/j.bmcl.2004.03.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  α-Azido ketones. Part 7: synthesis of 1,4-disubstituted triazoles by the "click" reaction of various terminal acetylenes with phenacyl azides or α-azidobenzo(hetera)cyclanones.

Authors:  Krisztina Kónya; Szabolcs Fekete; Anita Abrahám; Tamás Patonay
Journal:  Mol Divers       Date:  2012-02-04       Impact factor: 2.943

2.  Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.

Authors:  Stanislav A Bakunov; Svetlana M Bakunova; Tanja Wenzler; Maedot Ghebru; Karl A Werbovetz; Reto Brun; Richard R Tidwell
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

3.  Neglected disease - african sleeping sickness: recent synthetic and modeling advances.

Authors:  Sarvesh K Paliwal; Ankita Narayan Verma; Shailendra Paliwal
Journal:  Sci Pharm       Date:  2011-05-10

4.  Synthesis, characterization, and biological activity of N-methyl-2-(1H-1,2,3-benzotriazol-1-y1)-3-oxobutan- ethioamide complexes with some divalent metal (II) ions.

Authors:  Nouria A Al-Awadi; Nadia M Shuaib; Alaa Abbas; Ahmed A El-Sherif; Ali El-Dissouky; Esmaeil Al-Saleh
Journal:  Bioinorg Chem Appl       Date:  2008       Impact factor: 7.778

5.  New 1,2,3-Triazoles from (R)-Carvone: Synthesis, DFT Mechanistic Study and In Vitro Cytotoxic Evaluation.

Authors:  Ali Oubella; Abdoullah Bimoussa; Abdellah N'ait Oussidi; Mourad Fawzi; Aziz Auhmani; Hamid Morjani; Abdelkhalek Riahi; M'hamed Esseffar; Carol Parish; Moulay Youssef Ait Itto
Journal:  Molecules       Date:  2022-01-25       Impact factor: 4.411

Review 6.  Two decades of the synthesis of mono- and bis-aminomercapto[1,2,4]triazoles.

Authors:  Sayed M Riyadh; Sobhi M Gomha
Journal:  RSC Adv       Date:  2020-07-01       Impact factor: 4.036

7.  New Pyrazine Conjugates: Synthesis, Computational Studies, and Antiviral Properties against SARS-CoV-2.

Authors:  Israa A Seliem; Adel S Girgis; Yassmin Moatasim; Ahmed Kandeil; Ahmed Mostafa; Mohamed A Ali; Mohamed S Bekheit; Siva S Panda
Journal:  ChemMedChem       Date:  2021-09-06       Impact factor: 3.540
  7 in total

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