Full metadata record

DC FieldValueLanguage
dc.contributor.author김희숙-
dc.contributor.author신민재-
dc.contributor.author이병호-
dc.contributor.author오광석-
dc.contributor.author추현아-
dc.contributor.author배애님-
dc.contributor.author노은주-
dc.contributor.author남길수-
dc.date.accessioned2015-12-03T02:08:31Z-
dc.date.available2015-12-03T02:08:31Z-
dc.date.issued201511-
dc.identifier.citationVOL 36, NO 11, 2621-2626-
dc.identifier.issn02532964-
dc.identifier.other45447-
dc.identifier.urihttp://pubs.kist.re.kr/handle/201004/50856-
dc.description.abstractIn a search for novel molecules to treat inflammatory disorders, we identified several compounds with inhibitory action against the IKK2 enzyme using in silico methods. Based on the virtual hit of compounds 1 and 2, a novel series of 2-phenylimino-5((5-phenylfuran-2-yl)methylene)thiazolidin-4-one derivatives was designed, synthesized, and evaluated for IKK2 inhibitory activity. Among the synthesized derivatives, compounds 17f and 19f showed good IKK2 inhibitory potency, which have 4-carboxaminophenyl on the 2-furan ring and a methoxy group on the phenylimino moiety at the 2-position of the core structure. The most potent compound was 2-(2,4-dimethoxyphenyl)imino-5((5(4-carboxaminophenyl)furan-2-yl)methylene)thiazolidin-4-one (19f, IC50 = 0.94 μM), which represents a synergic effect of the two virtual hit compounds against IKK2. We also identified compounds showing inhibitory activities against interleukin (IL)-17, CCK-8, and tumor necrosis factor-alpha (TNF-α), which are NF-κB-dependent pro-inflammatory cytokine mediators.-
dc.publisherBulletin of the Korean Chemical Society-
dc.subject2-Phenylimino-5((5-phenylfuran-2-yl)methylene)thiazolidin-4-one-
dc.subjectIKK2-
dc.subjectAnti-inflammatiory activity-
dc.titleSynthesis and Biologicak Evaluation of 2-Phenylimino-5((5-phenylfuran-2-yl)methylene)thiazolidin-4-ones as IKK2 inhibitors-
dc.typeArticle-
Appears in Collections:
KIST Publication > Article
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