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Title 

Development of novel 1,2,3,4-tetrahydroquinoline scaffolds as potent NF-κB inhibitors and cytotoxic agents

Authors 

H JoM ChoiA S KumarY JungS KimJieun YunJong Soon KangY KimS B HanJ K JungJ ChoK LeeJ H KwakH Lee

Publisher 

American Chemical Society

Issue Date 

2016

Citation 

ACS Medicinal Chemistry Letters, vol. 7, no. 4, pp. 385-390

Keywords 

1,2,3,4-Tetrahydroquinolineshuman cancer cell linesin vitro cytotoxicityNF-κB inactivation

Abstract 

1,2,3,4-Tetrahydroquinolines have been identified as the most potent inhibitors of LPS-induced NF-κB transcriptional activity. To discover new molecules of this class with excellent activities, we designed and synthesized a series of novel derivatives of 1,2,3,4-tetrahydroquinolines (4a-g, 5a-h, 6a-h, and 7a-h) and bioevaluated their in vitro activity against human cancer cell lines (NCI-H23, ACHN, MDA-MB-231, PC-3, NUGC-3, and HCT 15). Among all synthesized scaffolds, 6g exhibited the most potent inhibition (53 times that of a reference compound) of LPS-induced NF-κB transcriptional activity and the most potent cytotoxicity against all evaluated human cancer cell lines.

ISSN 

1948-5875

Link 

http://dx.doi.org/10.1021/acsmedchemlett.6b00004

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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