166975-76-4Relevant articles and documents
A novel salicylic acid derivatives preparation method and its application in treating the tumor
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, (2019/04/10)
The invention belongs to the field of biological medicine, and particularly provides a novel salicylic acid derivatives and application in treating the tumor. We use the chemical synthetic method has been a series of novel salicylic acid derivatives of the compound. We found that the biological activity of the compounds to identify breast cancer, lung cancer, leukemia and other various cell strain has obvious antagonistic effect, we study found that anti-tumor mechanism of the class of compounds STAT3 cell signal transduction have prominent inhibit function, the display of these compounds for the treatment of STAT3 signal conduction abnormality types of cancer has a great significance.
Evolution from a natural flavones nucleus to obtain 2-(4-propoxyphenyl) quinoline derivatives as potent inhibitors of the S. aureus NorA efflux pump
Sabatini, Stefano,Gosetto, Francesca,Manfroni, Giuseppe,Tabarrini, Oriana,Kaatz, Glenn W.,Patel, Diixa,Cecchetti, Violetta
, p. 5722 - 5736 (2011/10/09)
Overexpression of efflux pumps is an important mechanism by which bacteria evade the effects of substrate antimicrobial agents. Inhibition of such pumps is a promising strategy to circumvent this resistance mechanism. NorA is a Staphylococcus aureus efflux pump that confers reduced susceptibility to many structurally unrelated agents, including fluoroquinolones, resulting in a multidrug resistant phenotype. In this work, a series of 2-phenyl-4(1H)- quinolone and 2-phenyl-4-hydroxyquinoline derivatives, obtained by modifying the flavone nucleus of known efflux pump inhibitors (EPIs), were synthesized in an effort to identify more potent S. aureus NorA EPIs. The 2-phenyl-4- hydroxyquinoline derivatives 28f and 29f display potent EPI activity against SA-1199B, a strain that overexpresses norA, in an ethidium bromide efflux inhibition assay. The same compounds, in combination with ciprofloxacin, were able to completely restore its antibacterial activity against both S. aureus SA-K2378 and SA-1199B, norA-overexpressing strains.
NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS
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Page/Page column 104-105, (2010/11/08)
The present invention is directed to novel tetracyclic heteroatom containing derivatives of formula (II), pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and proces
