612-34-0Relevant articles and documents
Highly selective and sensitive long fluorescence lifetime polyurethane foam sensor based on Tb-complex as chromophore for the detection of H2PO4 ? in water
, ()
Developing novel rare-earth complexes to rapidly and reliably sensing anions in pure water is highly challenging. Here, a series of long fluorescence lifetime polyurethane foam bonded Tb(BAA)3 chromophore porous material (Tb-PUFs) have been designed and synthesized via a simple one-step co-polycondensation reaction as an efficient fluorescent sensor for H2PO4 ? in pure water. All Tb-PUFs exhibited strong green emission and long fluorescence lifetime in water, which was ascribed to Tb-complex can be dispersed very well in polyurethane foam, effectively avoiding the emission quenching of Tb3+ ions caused by water molecules vibration. The titration experimental results showed that precursor Tb(BAA)3 can effective recognize F?, CH3COO?, and H2PO4 ? in DMSO solution. Interestingly, Tb-PUFs can only selectively recognize H2PO4 ? in pure water, this phenomenon can be explained that H2PO4 ? is acidic, and can occur deprotonation with -NH group of ligand BAA, thus making the fluorescence quenching effect was more sensitive for H2PO4 ? in pure water. In addition, the sensing ability of Tb-PUFs for H2PO4 ? is highly reversible by washing them with deionized water for three times. In a word, all results implied that Tb-PUFs was an excellent candidate for H2PO4 ? ions detection selectively in pure water.
Halogen-substituted anthranilic acid derivatives provide a novel chemical platform for androgen receptor antagonists
Roell, Daniela,R?sler, Thomas W.,Hessenkemper, Wiebke,Kraft, Florian,Hauschild, Monique,Bartsch, Sophie,Abraham, Tsion E.,Houtsmuller, Adriaan B.,Matusch, Rudolf,van Royen, Martin E.,Baniahmad, Aria
, p. 59 - 70 (2019/02/01)
Androgen receptor (AR) antagonists are used for hormone therapy of prostate cancer (PCa). However resistance to the treatment occurs eventually. One possible reason is the occurrence of AR mutations that prevent inhibition of AR-mediated transactivation by antagonists. To offer in future more options to inhibit AR signaling, novel chemical lead structures for new AR antagonists would be beneficial. Here we analyzed structure-activity relationships of a battery of 36 non-steroidal structural variants of methyl anthranilate including 23 synthesized compounds. We identified structural requirements that lead to more potent AR antagonists. Specific compounds inhibit the transactivation of wild-type AR as well as AR mutants that render treatment resistance to hydroxyflutamide, bicalutamide and the second-generation AR antagonist enzalutamide. This suggests a distinct mode of inhibiting the AR compared to the clinically used compounds. Competition assays suggest binding of these compounds to the AR ligand binding domain and inhibit PCa cell proliferation. Moreover, active compounds induce cellular senescence despite inhibition of AR-mediated transactivation indicating a transactivation-independent AR-pathway. In line with this, fluorescence resonance after photobleaching (FRAP) - assays reveal higher mobility of the AR in the cell nuclei. Mechanistically, fluorescence resonance energy transfer (FRET) - assays indicate that the amino-carboxy (N/C)-interaction of the AR is not affected, which is in contrast to known AR-antagonists. This suggests a mechanistically novel mode of AR-antagonism. Together, these findings indicate the identification of a novel chemical platform as a new lead structure that extends the diversity of known AR antagonists and possesses a distinct mode of antagonizing AR-function.
Convenient and sequential one-pot route for synthesis of 2-thioxoquinazolinone and quinazolinobenzothiazinedione derivatives
Asadi, Mehdi,Masoomi, Shiva,Ebrahimi, Seyed Mostafa,Mahdavi, Mohammad,Saeedi, Mina,Shafiee, Abbas,Foroumadi, Alireza
, p. 497 - 504 (2014/03/21)
A new and efficient synthetic process has been developed for preparation of 2-thioxoquinazolinone and quinazolinobenzothiazinedione derivatives. The related products were synthesized through reaction of isatoic anhydride, amines/anthranilic acids, and carbon disulfide (CS2) in the presence of potassium hydroxide in ethanol at reflux. Graphical abstract: [Figure not available: see fulltext.]
