57543-67-6Relevant articles and documents
3-nitro-2H-chromenes as a new class of inhibitors against thioredoxin reductase and proliferation of cancer cells
Xiao, Guo-Qiang,Liang, Bao-Xia,Chen, Shu-Han,Ou, Tian-Miao,Bu, Xian-Zhang,Yan, Ming
, p. 767 - 770 (2012)
A series of 3-nitrochromenes were designed and synthesized. These compounds showed good inhibitory activity against thioredoxin reductase (TrxR) and the proliferation of A549 cancer cells. The structure-activity relationship analysis indicates that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. The bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity. A series of 3-nitrochromenes were designed and synthesized. They showed good inhibitory activity against thioredoxin reductase and the proliferation of A549 cancer cells. Structure-activity relationship analysis revealed that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. Bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity. Copyright
Microwave-Assisted Rapid and Efficient Synthesis of New Series of Chromene-Based 1,2,4-Oxadiazole Derivatives and Evaluation of Antibacterial Activity with Molecular Docking Investigation
Baral, Nilofar,Mohapatra, Seetaram,Raiguru, Bishnu Prasad,Mishra, Nilima Priyadarsini,Panda, Pravati,Nayak, Sabita,Pandey, Satyendra Kumar,Kumar, P. Sudhir,Sahoo, Chita Ranjan
, p. 552 - 565 (2019/01/04)
A new series of novel chromene-based oxadiazole derivatives were synthesized from a variety of chromene-based amidoximes with readily available carboxylic acids under conventional oil bath heating as well as under microwave irradiation. The use of commercially available EDCI and HOBt as coupling reagents in DMF combined with microwave heating resulted in high yields and purities of the product 1,2,4-oxadiazoles in an expeditious manner. This methodology is successfully applied to synthesize 18 numbers of new 2H-chromene-substituted 1,2,4-oxadiazole derivatives in good to high yields. The structure of the product was ascertained by X-ray crystallographic analysis. All the synthesized compounds were evaluated for their in vitro antibacterial activity against two different pathogenic bacterial strains, that is, Escherichia coli (MTCC614) and Klebsiella pneumoniae (MTCC4031). The obtained results from in vitro antimicrobial assays indicated that 6g and 6h exhibited good antibacterial activity nearer to the standard drug, gentamicin. The molecular docking studies showed that compounds 6g and 6h show hydrogen bonding interaction with the bacterial target DNA gyrase of E.?coli.
DUAL AGONISTS OF FXR AND PPARδ AND THEIR USES
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Page/Page column 38; 46, (2019/04/16)
The present invention relates to small molecule compounds and their use as agonists of farnesoid X receptor (FXR) and/or peroxisome proliferator activated receptor delta (PPARδ). The present invention also relates to the use of said compounds in the treatment of metabolic diseases and respective methods of treatment.