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

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Title
Design and synthesis of 3,4-dihydro-2H-benzo[h]chromene derivatives as potential NF-κB inhibitors
Author(s)
M Choi; Y S Hwang; A S Kumar; H Jo; Y Jeong; Y Oh; J Lee; Jieun Yun; Y Kim; S B Han; J K Jung; J Cho; H Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 11, pp. 2404-2407
Publication Year
2014
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.
Keyword
Cytotoxic activityN-Aryl-3,4-dihydro-2H-benzo[h] chromene-2-caboxamide derivativesNF-κB inhibitors
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2014.04.053
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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