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Title 

Design and synthesis of 2,3-dihydro- and 5-chloro-2,3-dihydro-naphtho-[1,2-b]furan-2-carboxylic acid N-(substitutedphenyl)amide analogs and their biological activities as inhibitors of NF-kB activity and anticancer agents

Authors 

M ChoiH JoD KimJi Eun YunJong Soon KangY KimJ K JungJ T HongJ ChoJ H KwakH Lee

Publisher 

Pharmaceutical Society of Korea

Issue Date 

2016

Citation 

Archives of Pharmacal Research, vol. 39, no. 5, pp. 618-630

Keywords 

2,3-Dihydronaphtho-[1,2-b]furan scaffoldsAnticancer activityInhibition of NF-κB transcriptional activity

Abstract 

A series of 2,3-dihydro- and 5-chloro-2,3-dihydro-naphtho-[1,2-b]furan-2-carboxylic acid N-(substitutedphenyl)amide analogs (1a?k and 2a?i) were designed and synthesized for developing novel naphthofuran scaffolds as anticancer agents and inhibitors of NF-κB activity. Compound 1d, which had a 4′-chloro group on the N-phenyl ring, exhibited inhibitory activity of NF-κB. Compound 2g, which had a 5′-chloro group on the naphthofuran ring and a 3′,5′-bistrifluoromethane group on the N-phenyl ring, had the best NF-κB inhibitory activity. In addition, the novel analogs exhibited potent cytotoxicity at low concentrations against HCT-116, NCI-H23, and PC-3 cell lines. The two electron-withdrawing groups, especially at the 3′,5′-position on the N-phenyl ring, increased anticancer activity and NF-κB inhibitory activity. However, only 5-chloro-2,3-dihydronaphtho[1,2-b]furan-2-carboxylic N-(3′,5′-bis(trifluoromethyl)phenyl)amide (2g) exhibited both outstanding cytotoxicity and NF-κB inhibitory activities. This novel lead scaffold may be helpful for investigation of new anticancer agents by inactivation of NF-κB.

ISSN 

0253-6269

Link 

http://dx.doi.org/10.1007/s12272-016-0737-5

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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