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Title 

Design and synthesis of 3,4-dihydro-2H-benzo[h]chromene derivatives as potential NF-κB inhibitors

Authors 

M ChoiY S HwangA S KumarH JoY JeongY OhJ LeeJieun YunY KimS B HanJ K JungJ ChoH Lee

Publisher 

Elsevier

Issue Date 

2014

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 11, pp. 2404-2407

Keywords 

Cytotoxic activityN-Aryl-3,4-dihydro-2H-benzo[h] chromene-2-caboxamide derivativesNF-κB inhibitors

Abstract 

A novel class of NF-κB inhibitors were designed and synthesized based on KL-1156 (6-hydroxy-7-methoxychroman-2-carboxylic acid phenyl amide) which is unambiguously considered to be a promising inhibitor for the translocation step of NF-κB. Especially in this study we focused on the modifying the chroman moiety of KL-1156 into four parts for exploring the SAR studies linked with physical properties of substituents resulted the development of novel 1a-k, 2a-f, 3a-d and 4a-d derivatives of 3,4-dihydro-2H-benzo[h]chromene. From the SAR studies we were very delightfully identified that several new N-aryl-3,4-dihydro-2H-benzo[h]chromene-2-carboxamide derivatives (1a-k) exhibited good inhibitory activity and anti-proliferative activity than parent lead compound KL-1156, among them 1i exhibited outstanding inhibitory effect on LPS-induced NF-κB transcriptional activity and anti-proliferative activity on NCI-H23 lung cancer cell lines than KL-1156.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2014.04.053

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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