1609235-46-2Relevant academic research and scientific papers
Design and synthesis of 3,4-dihydro-2H-benzo[h]chromene derivatives as potential NF-κB inhibitors
Choi, Minho,Hwang, Young-Sik,Kumar, Arepalli Sateesh,Jo, Hyeju,Jeong, Yeongeun,Oh, Yunju,Lee, Joonkwang,Yun, Jieun,Kim, Youngsoo,Han, Sang-Bae,Jung, Jae-Kyung,Cho, Jungsook,Lee, Heesoon
supporting information, p. 2404 - 2407 (2014/05/20)
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.
