374768-02-2Relevant articles and documents
Synthesis and bioactivity of novel coumarin derivatives
Zhang, Sai-Yang,Fu, Dong-Jun,Sun, Hui-Hui,Yue, Xiao-Xin,Liu, Ying-Chao,Zhang, Yan-Bing,Liu, Hong-Min
, p. 374 - 378 (2017/03/16)
[Figure not available: see fulltext.] A series of novel coumarin derivatives were synthesized from commercially available chemical agents. All prepared compounds were evaluated for their in vitro antiproliferative activity against five selected human cancer cell lines (EC109, MGC-803, PC-3, MCF-7, and EC9706) and their in vitro antimicrobial activity against E. coli and M. albicans. 4-(3-Bromopropoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MGC-803 cell line (IC50 47.7 μM) and 7-(2-bromoethoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MCF-7 cell line (IC50 48.3 μM). The latter compound was also the most active against E. coli (MIC50 0.27 μg/ml).
Synthesis and Biological Evaluation of ortho-Aryl N-Hydroxycinnamides as Potent Histone Deacetylase (HDAC) 8 Isoform-Selective Inhibitors
Huang, Wei-Jan,Wang, Yi-Ching,Chao, Shi-Wei,Yang, Chen-Yui,Chen, Liang-Chieh,Lin, Mei-Hsiang,Hou, Wen-Chi,Chen, Mei-Yu,Lee, Tai-Lin,Yang, Ping,Chang, Chung-I
, p. 1815 - 1824 (2012/10/29)
Histone deacetylases (HDACs) are a family of enzymes that play a crucial role in biological process and diseases. In contrast to other isozymes, HDAC8 is uniquely incapable of histone acetylation. In order to delineate its physiological function, we devel
Inhibitory effects of 6-alkoxycoumarin and 7-alkoxycoumarin derivatives on lipopolysaccharide/interferon γ-stimulated nitric oxide production in RAW264 cells
Adfa, Morina,Itoh, Tomohiro,Hattori, Yosuke,Koketsu, Mamoru
experimental part, p. 963 - 966 (2012/09/21)
Coumarin and its derivatives are well known for their anti-inflammatory and anti-oxidative effects. In this study, we synthesized 32 coumarin derivatives from commercially available 6-hydroxycoumarin (6HC) and 7-hydroxycoumarin (7HC) and examined their ef
Structure-activity relationships for naturally occurring coumarins as β-secretase inhibitor
Marumoto, Shinsuke,Miyazawa, Mitsuo
supporting information; experimental part, p. 784 - 788 (2012/03/22)
The present study was demonstrated to evaluate the effects of naturally occurring coumarins (NOCs) including simple coumarins, furanocoumarins, and pyranocoumarins on the inhibition of β-secretase (BACE1) activity. Of 41 NOCs examined, some furanocoumarins inhibited BACE1 activity, but simple coumarins and pyranocoumarins did not affect. The most potent inhibitor was 5-geranyloxy-8-methoxypsoralen (31), which has an IC50 value of 9.9 μM. Other furanocoumarin derivatives, for example, 8-geranyloxy-5- methoxypsoralen (35), 8-geranyloxypsoralen (24), and bergamottin (18) inhibited BACE1 activity, with the IC50 values 25.0 μM. Analyses of the inhibition mechanism by Dixon plots and Cornish-Bowden plots showed that compounds 18, 31 and 35 were mixed-type inhibitor. The kinetics of inhibition of BACE1 by coumarins 24 was non-competitive inhibitors.