4252-99-7Relevant academic research and scientific papers
Discovery of human TyrRS inhibitors by structure-based virtual screening, structural optimization, and bioassays
Huang, Shenzhen,Wang, Xiang,Lin, Guifeng,Cheng, Jie,Chen, Xiuli,Sun, Weining,Xiang, Rong,Yu, Yamei,Li, Linli,Yang, Shengyong
, p. 9323 - 9330 (2019/03/28)
The human tyrosyl transfer-RNA (tRNA) synthetase (TyrRS), which is well known for its essential aminoacylation function in protein synthesis, has been shown to translocate to the nucleus and protect against DNA damage caused by external stimuli. Small molecules that can fit into the active site pocket of TyrRS are thought to affect the nuclear role. The exploitation of TyrRS inhibitors has attracted attention recently. In this investigation, we adopted a structure-based virtual screening strategy and subsequent structure-activity relationship analysis to discover new TyrRS inhibitors, and identified a potent compound 5,7-dihydroxy-6,8-bis((3-hydroxyphenyl)thio)-2-phenyl-4H-chromen-4-one (compound 11, Ki = 8.8 μM). In intact HeLa cells, this compound showed a protective effect against DNA damage. Compound 11 is a good lead compound for the further development of drugs against disorders caused by DNA damage.
Substituted 6,8-dimercapto-2-phenyl-4H-chromen-4-one derivative and preparation method and application thereof
-
Paragraph 0027; 0032; 0033; 0034, (2018/11/03)
The invention belongs to the field of organic synthetic medicine and particularly relates to a substituted 6,8-dimercapto-2-phenyl-4H-chromen-4-one derivative, having the structure that is shown in the description. Embodiments of the substituted 6,8-dimercapto-2-phenyl-4H-chromen-4-one derivative prove that the derivative can activate TyrRS-PARP-1 signal pathway such that activation of PARP-1 viaTyrRS leads to a series of protective genes, including tumor inhibiting gene p53 and longevity genes FOXO3A and SIRT6 to be activated; the derivative has good medicinal potential in age defying and DNA restoration drugs, and a new potential option is provided for clinical medication; in addition, a preparation method of a new compound herein is simple, the preparation method has mild reaction conditions, is convenient to perform and control, has low energy consumption, high yield and low cost, and is suitable for industrial production, and the compound produced has high bioactivity, high activity and selectivity, significant drug-likeness, and promising market prospect.
6,8-Dibromo- and 6,8-Diiodo-5,7-dihydroxyflavones as New Potent Antibacterial Agents
Kingkaew, Krongkan,Ruga, Ritbey,Chavasiri, Warinthorn
supporting information, p. 258 - 261 (2018/03/01)
Thirteen flavones including chrysin, three natural and nine synthesized compounds, were examined for antibacterial activity. 6,8-Dibromo- (11) and 6,8-diiodo-5,7-dihydroxyflavone (12) exhibited the highest activity against all bacteria with MIC 31.2562.5
Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives
Park, Haeil,Tran, Thanh Dao,Hyun, Pyo Kim
, p. 943 - 948 (2007/10/03)
A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE2 inhibitory activities. 6,8-Disubstituted chrysin derivatives were obtained from naturally occurring chrysin by halogenation, oxidation, thiomet
An efficient approach to dihydrofuroflavonoids via palladium-catalyzed annulation of 1,3-dienes by 0-iodoacetoxyflavonoids
Rozhkov, Roman V.,Larock, Richard C.
, p. 1854 - 1858 (2007/10/03)
The palladium-catalyzed annulation of 1,3-dienes by o-iodoacetoxyflavonoids provides an efficient approach to biologically interesting dihydrofuroflavonoids. This reaction is very general, stereo-and regioselective, and a wide variety of terminal, cyclic and internal 1,3-dienes can be utilized.
Plasminogen activator inhibitor antagonists
-
, (2008/06/13)
Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl et
Synthesis and anticancer effect of chrysin derivatives
Zheng, Xing,Meng, Wei-Dong,Xu, Yang-Yan,Cao, Jian-Guo,Qing, Feng-Ling
, p. 881 - 884 (2007/10/03)
A series of chrysin derivatives, prepared by alkylation, halogenation, nitration, methylation, acetylation and trifluoromethylation, were tested in vitro against human gastric adenocarcinoma cell line (SGC-7901) and colorectal adenocarcinoma (HT-29) cells. Among these derivatives of chrysin, 5,7-dimethoxy-8-iodochrysin 3 and 8-bromo-5-hydroxy-7-methoxychrysin 11 have the strongest activities against SGC-7901 and HT-29 cells, respectively. 5,7-Dihydroxy-8-nitrochrysin 12 were found to have strong activities against both SGC-7901 and HT-29 cells.
