View : 198 Download: 0

Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors

Title
Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors
Authors
Park, Myoung-SoonPark, Hyun-JuAn, Young JaeChoi, Joon HunCha, GeunyoungLee, Hwa JeongPark, So-JungDewang, Purushottam M.Kim, Dae-Kee
Ewha Authors
이화정김대기
SCOPUS Author ID
이화정scopusscopus; 김대기scopus
Issue Date
2020
Journal Title
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
ISSN
1475-6366JCR Link

1475-6374JCR Link
Citation
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY vol. 35, no. 1, pp. 702 - 712
Keywords
24-Disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazolesALK5 inhibitioncancer immunotherapeutic agentdocking
Publisher
TAYLOR &

FRANCIS LTD
Indexed
SCIE; SCOPUS WOS
Document Type
Article
Abstract
A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles, 7a-c, 11a-h, and 16a-h has been synthesised and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Incorporation of a quinoxalin-6-yl moiety and a methylene linker at the 4- and 2-position of the imidazole ring, respectively, and a m-CONH2 substituent in the phenyl ring generated a highly potent and selective ALK5 inhibitor 11e. Docking model of ALK5 in complex with 11e showed that it fitted well in the ATP-binding pocket with favourable interactions.
Show the fulltext
DOI
10.1080/14756366.2020.1734799
Appears in Collections:
약학대학 > 약학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE